Target Information

Target General Information

Top

Target ID

T67162 (Former ID: TTDS00012)

Target Name

Dopamine D2 receptor (D2R)

Synonyms

Dopamine receptor 2; D(2) dopamine receptor

Click to Show/Hide

Gene Name

DRD2

Target Type

Successful target

[1]

Disease

[+] 33 Target-related Diseases

Allergic/hypersensitivity disorder [ICD-11: 4A80-4A8Z]

Alzheimer disease [ICD-11: 8A20]

Asthma [ICD-11: CA23]

Attention deficit hyperactivity disorder [ICD-11: 6A05]

Bipolar disorder [ICD-11: 6A60]

Breathing abnormality [ICD-11: MD11]

Cardiovascular disease [ICD-11: BA00-BE2Z]

Cerebral ischaemia [ICD-11: 8B1Z]

Depression [ICD-11: 6A70-6A7Z]

Digestive system disease [ICD-11: DE2Z]

Essential hypertension [ICD-11: BA00]

Faecal incontinence [ICD-11: ME07]

Gangrene [ICD-11: MC85]

Glaucoma [ICD-11: 9C61]

Heart failure [ICD-11: BD10-BD1Z]

Hyperaemia [ICD-11: 9A61-9B7Y]

Hypertension [ICD-11: BA00-BA04]

Hypotension [ICD-11: BA20-BA21]

Inborn porphyrin/heme metabolism error [ICD-11: 5C58]

Insomnia [ICD-11: 7A00-7A0Z]

Itching [ICD-11: 1F28-1G07]

Migraine [ICD-11: 8A80]

Nausea/vomiting [ICD-11: MD90]

Pain [ICD-11: MG30-MG3Z]

Parkinsonism [ICD-11: 8A00]

Pituitary gland disorder [ICD-11: 5A60-5A61]

Postpartum haemorrhage [ICD-11: JA43]

Psychotic disorder [ICD-11: 6A20-6A25]

Pulmonary hypertension [ICD-11: BB01]

Schizophrenia [ICD-11: 6A20]

Substance abuse [ICD-11: 6C40]

Thyrotoxicosis [ICD-11: 5A02]

Type 2 diabetes mellitus [ICD-11: 5A11]

Function

Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.

Click to Show/Hide

BioChemical Class

GPCR rhodopsin

UniProt ID

DRD2_HUMAN

Sequence

MDPLNLSWYDDDLERQNWSRPFNGSDGKADRPHYNYYATLLTLLIAVIVFGNVLVCMAVS
REKALQTTTNYLIVSLAVADLLVATLVMPWVVYLEVVGEWKFSRIHCDIFVTLDVMMCTA
SILNLCAISIDRYTAVAMPMLYNTRYSSKRRVTVMISIVWVLSFTISCPLLFGLNNADQN
ECIIANPAFVVYSSIVSFYVPFIVTLLVYIKIYIVLRRRRKRVNTKRSSRAFRAHLRAPL
KGNCTHPEDMKLCTVIMKSNGSFPVNRRRVEAARRAQELEMEMLSSTSPPERTRYSPIPP
SHHQLTLPDPSHHGLHSTPDSPAKPEKNGHAKDHPKIAKIFEIQTMPNGKTRTSLKTMSR
RKLSQQKEKKATQMLAIVLGVFIICWLPFFITHILNIHCDCNIPPVLYSAFTWLGYVNSA
VNPIIYTTFNIEFRKAFLKILHC

Click to Show/Hide

3D Structure

Click to Show 3D Structure of This Target

PDB

ADReCS ID

BADD_A03272 ; BADD_A04234

HIT2.0 ID

T48ZIG

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 58 Approved Drugs

Acetophenazine

Drug Info

Approved

Bipolar disorder

[2], [16]

Amisulpride

Drug Info

Approved

Schizophrenia

[14], [17]

Aniracetam

Drug Info

Approved

Cerebrovascular ischaemia

[18], [19]

Apomorphine

Drug Info

Approved

Parkinson disease

[20], [21]

Aripiprazole

Drug Info

Approved

Schizophrenia

[22], [23]

Bevantolol

Drug Info

Approved

Hypertension

[2], [14]

Bromocriptine

Drug Info

Approved

Parkinson disease

[24], [25]

Cabergoline

Drug Info

Approved

Hyperprolactinaemia

[25], [26]

Cariprazine

Drug Info

Approved

Bipolar disorder

[27], [28]

Carphenazine

Drug Info

Approved

Insomnia

[2]

Chlorprothixene

Drug Info

Approved

Psychotic disorder

[29]

Dapiprazole

Drug Info

Approved

Glaucoma/ocular hypertension

[2]

Denopamine

Drug Info

Approved

Cardiac disease

[2], [30]

Dihydroergotoxine

Drug Info

Approved

Alzheimer disease

[31]

Docarpamine

Drug Info

Approved

Hypertension

[2]

Domperidone

Drug Info

Approved

Gastrointestinal disease

[32], [33]

Dopamine

Drug Info

Approved

Parkinson disease

[34], [35]

Droperidol

Drug Info

Approved

Nausea

[36], [37]

Ephedrine

Drug Info

Approved

Asthma

[38], [39]

Ergonovine

Drug Info

Approved

Postpartum haemorrhage

[40], [41]

Haloperidol

Drug Info

Approved

Schizophrenia

[14], [42]

Iloperidone

Drug Info

Approved

Schizophrenia

[43], [44]

Levodopa

Drug Info

Approved

Parkinson disease

[45]

Levomepromazine

Drug Info

Approved

Psychotic disorder

[2]

Lurasidone hydrochloride

Drug Info

Approved

Schizophrenia

[2], [46], [47], [48]

Meglitinides

Drug Info

Approved

Type-2 diabetes

[49]

Mephentermine

Drug Info

Approved

High blood pressure

[2]

Mesoridazine

Drug Info

Approved

Schizophrenia

[50], [51]

Metaraminol

Drug Info

Approved

Hypotension

[52], [53]

Methamphetamine

Drug Info

Approved

Pain

[54]

Methyldopa

Drug Info

Approved

Hypertension

[55], [56]

Metoclopramide

Drug Info

Approved

Nausea

[57], [58]

Molindone

Drug Info

Approved

Schizophrenia

[59], [60]

N-0923

Drug Info

Approved

Parkinson disease

[61], [62]

Naphazoline

Drug Info

Approved

Itching

[2]

Nemonapride

Drug Info

Approved

Schizophrenia

[63], [35]

OPC-34712

Drug Info

Approved

Major depressive disorder

[64], [65]

Perazine

Drug Info

Approved

Psychotic disorder

[2]

Pergolide

Drug Info

Approved

Parkinson disease

[66], [25]

Perphenazine

Drug Info

Approved

Schizophrenia

[67], [68]

Phentolamine

Drug Info

Approved

Dermal necrosis

[69], [70]

Phenylephrine

Drug Info

Approved

Fecal incontinence

[71]

Phenyltoloxamine

Drug Info

Approved

Allergy

[2]

Pimozide

Drug Info

Approved

Schizophrenia

[72], [73]

Piperacetazine

Drug Info

Approved

Schizophrenia

[2]

Pramipexole

Drug Info

Approved

Parkinson disease

[74], [75]

Prochlorperazine

Drug Info

Approved

Nausea

[76], [77]

Pseudoephedrine

Drug Info

Approved

Nasal congestion

[78], [79]

Quetiapine

Drug Info

Approved

Schizophrenia

[35], [80], [81]

Risperidone

Drug Info

Approved

Schizophrenia

[82], [83]

Ropinirole

Drug Info

Approved

Parkinson disease

[84], [85]

Sulpiride

Drug Info

Approved

Schizophrenia

[86], [87]

Thioridazine

Drug Info

Approved

Schizophrenia

[88], [89]

Thiothixene

Drug Info

Approved

Schizophrenia

[90], [91]

Tiapride

Drug Info

Approved

Alcohol dependence

[2]

Tolazoline

Drug Info

Approved

Pulmonary hypertension

[92], [93], [2]

Ziprasidone

Drug Info

Approved

Schizophrenia

[35], [94], [83]

Zuclopenthixol

Drug Info

Approved

Schizophrenia

[95], [96]

Clinical Trial Drug(s)

[+] 37 Clinical Trial Drugs

Bis(olanzapine) pamoate monohydrate

Drug Info

Phase 3

Psychotic disorder

[2]

Blonanserin

Drug Info

Phase 3

Schizophrenia

[98], [35]

CQA 206-291

Drug Info

Phase 3

Parkinson disease

[99]

Entacapone+levodopa+carbidopa

Drug Info

Phase 3

Restless legs syndrome

[100]

Lu AF35700

Drug Info

Phase 3

Schizophrenia

[101]

P2B-001

Drug Info

Phase 3

Parkinson disease

[102]

Pridopidine

Drug Info

Phase 3

Huntington disease

[103]

RBP-7000

Drug Info

Phase 3

Non-small-cell lung cancer

[104]

Sumanirole

Drug Info

Phase 3

Parkinson disease

[105], [106]

Zicronapine

Drug Info

Phase 3

Schizophrenia

[107]

APD-403

Drug Info

Phase 2

Vomiting

[111]

BIM23A760

Drug Info

Phase 2

Acromegaly

[112], [113]

BL-1020

Drug Info

Phase 2

Schizophrenia

[35]

CGS-15873A

Drug Info

Phase 2

Psychotic disorder

[114]

CLR-3001

Drug Info

Phase 2

Major depressive disorder

[115]

JNJ-37822681

Drug Info

Phase 2

Schizophrenia

[116]

Mazapertine succinate

Drug Info

Phase 2

Psychotic disorder

[117]

Ocaperidone

Drug Info

Phase 2

Schizoaffective disorder

[118], [35], [119]

ONC201

Drug Info

Phase 2

Glioma

[120], [102]

Pardoprunox

Drug Info

Phase 2

Parkinson disease

[75]

PD-143188

Drug Info

Phase 2

Psychotic disorder

[121]

ROXINDOLE

Drug Info

Phase 2

Psychotic disorder

[122], [123]

RP5063

Drug Info

Phase 2

Schizophrenia

[124]

SDZ-MAR-327

Drug Info

Phase 2

Psychotic disorder

[35], [125]

XP-21279

Drug Info

Phase 2

Parkinson disease

[126]

(-)-3PPP, Maryland

Drug Info

Phase 1

Schizophrenia

[129]

1192U90

Drug Info

Phase 1

Psychotic disorder

[130]

Abaperidone

Drug Info

Phase 1

Schizophrenia

[131]

ATI-9242

Drug Info

Phase 1

Schizophrenia

[101]

Carmoxirole

Drug Info

Phase 1

Hypertension

[132]

DSP-1200

Drug Info

Phase 1

Depression

[101]

Lu-02-750

Drug Info

Phase 1

Parkinson disease

[133]

Lu-AE04621

Drug Info

Phase 1

Parkinson disease

[134]

SKL-10406

Drug Info

Phase 1

Major depressive disorder

[135]

SSR-181507

Drug Info

Phase 1

Schizophrenia

[35]

Umespirone

Drug Info

Phase 1

Anxiety disorder

[136]

YKP-1358

Drug Info

Phase 1

Schizoaffective disorder

[35]

Patented Agent(s)

[+] 3 Patented Agents

PMID30124346-Compound-13TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[137]

PMID30124346-Compound-34TABLE4

Drug Info

Patented

Attention deficit hyperactivity disorder

[137]

PMID30124346-Compound-60TABLE5

Drug Info

Patented

Parkinson disease

[138], [139], [137]

Discontinued Drug(s)

[+] 41 Discontinued Drugs

Fencamfamine

Drug Info

Withdrawn from market

Depressive fatigue

[140]

Flupenthixol

Drug Info

Withdrawn from market

Schizophrenia

[141], [142]

Nomifensine

Drug Info

Withdrawn from market

Breast cancer

[143], [2]

Remoxipride

Drug Info

Withdrawn from market

Schizophrenia

[144]

Sertindole

Drug Info

Withdrawn from market

Schizophrenia

[145], [146]

(S)-amisulpride

Drug Info

Discontinued in Phase 4

Schizophrenia

[35]

Bifeprunox

Drug Info

Discontinued in Phase 3

Schizophrenia

[35]

Lamectacin

Drug Info

Discontinued in Phase 3

Bacterial infection

[147]

NOLOMIROLE HYDROCHLORIDE

Drug Info

Discontinued in Phase 3

Heart failure

[148]

Sibenadet

Drug Info

Discontinued in Phase 3

Chronic obstructive pulmonary disease

[149]

BAM-1110

Drug Info

Discontinued in Phase 2

Parkinson disease

[151]

Declopramide

Drug Info

Discontinued in Phase 2

Inflammatory bowel disease

[152]

Naxagolide

Drug Info

Discontinued in Phase 2

Parkinson disease

[153]

PF-217830

Drug Info

Discontinued in Phase 2

Schizophrenia

[154]

Romergoline

Drug Info

Discontinued in Phase 2

Anxiety disorder

[155]

SAVOXEPIN MESYLATE

Drug Info

Discontinued in Phase 2

Psychotic disorder

[156]

SLV-310

Drug Info

Discontinued in Phase 2

Schizophrenia

[35]

AM-831

Drug Info

Discontinued in Phase 1

Schizophrenia

[157]

DU-29894

Drug Info

Discontinued in Phase 1

Psychotic disorder

[158]

Ordopidine

Drug Info

Discontinued in Phase 1

Psychotic disorder

[159]

S-18327

Drug Info

Discontinued in Phase 1

Psychotic disorder

[160]

SDZ-GLC-756

Drug Info

Discontinued in Phase 1

Glaucoma/ocular hypertension

[161]

SLV-313

Drug Info

Discontinued in Phase 1

Schizophrenia

[35]

A-68930

Drug Info

Terminated

Hypertension

[166], [167]

AMR-103

Drug Info

Terminated

Parkinson disease

[168]

BIMG80

Drug Info

Terminated

Psychotic disorder

[169]

CGP-25454A

Drug Info

Terminated

Major depressive disorder

[170]

CP-903397

Drug Info

Terminated

Schizophrenia

[171]

Dianicline+rimonabant

Drug Info

Terminated

Tobacco dependence

[172]

E-2040

Drug Info

Terminated

Schizophrenia

[173]

Etrabamine

Drug Info

Terminated

Parkinson disease

[174]

GMC-283

Drug Info

Terminated

Schizophrenia

[35]

LY-243062

Drug Info

Terminated

Inflammation

[175]

NGD-93-1

Drug Info

Terminated

Psychotic disorder

[176]

NNC-22-0031

Drug Info

Terminated

Psychotic disorder

[177]

Org-10490

Drug Info

Terminated

Psychotic disorder

[178]

PNU-96391A

Drug Info

Terminated

Substance use disorder

[179]

RWJ-25730

Drug Info

Terminated

Psychotic disorder

[180]

Y-20024

Drug Info

Terminated

Psychotic disorder

[181]

Y-931

Drug Info

Terminated

Schizophrenia

[35]

ZD-3638

Drug Info

Terminated

Schizophrenia

[35]

Preclinical Drug(s)

[+] 6 Preclinical Drugs

F-15063

Drug Info

Preclinical

Schizophrenia

[162]

Org-23366

Drug Info

Preclinical

Schizophrenia

[35]

PD-157695

Drug Info

Preclinical

Schizophrenia

[35]

PD-158771

Drug Info

Preclinical

Schizophrenia

[35]

PGX-200097

Drug Info

Preclinical

Schizophrenia

[163]

S32504

Drug Info

Preclinical

Parkinson disease

[164]

Mode of Action

[+] 8 Modes of Action

Antagonist

[+] 49 Antagonist drugs

Acetophenazine

Drug Info

[182], [183]

Amisulpride

Drug Info

[182], [184], [185]

Bevantolol

Drug Info

[189], [190]

Carphenazine

Drug Info

[182], [195]

Chlorprothixene

Drug Info

[196]

Dapiprazole

Drug Info

[197]

Domperidone

Drug Info

[198], [199]

Haloperidol

Drug Info

[204], [182]

Iloperidone

Drug Info

[44], [35]

Meglitinides

Drug Info

[206], [207]

Metoclopramide

Drug Info

[212], [199]

Perphenazine

Drug Info

[219], [220]

Phentolamine

Drug Info

[221]

Pimozide

Drug Info

[225], [182]

Prochlorperazine

Drug Info

[226], [227]

Risperidone

Drug Info

[231], [232]

Sulpiride

Drug Info

[207], [233], [234]

Thioridazine

Drug Info

[235], [236]

Thiothixene

Drug Info

[237]

Tiapride

Drug Info

[233]

Tolazoline

Drug Info

[238]

Zuclopenthixol

Drug Info

[240], [182]

Blonanserin

Drug Info

[35]

APD-403

Drug Info

[248]

BL-1020

Drug Info

[35]

ONC201

Drug Info

[120]

RP5063

Drug Info

[255], [256]

1192U90

Drug Info

[35]

DSP-1200

Drug Info

[101]

Umespirone

Drug Info

[266]

L-piperazino-3-phenyl-indane derivative 1

Drug Info

[269]

Flupenthixol

Drug Info

[271], [182]

Nomifensine

Drug Info

[272], [273]

Remoxipride

Drug Info

[182], [274]

Sertindole

Drug Info

[275], [276]

(S)-amisulpride

Drug Info

[35]

Lamectacin

Drug Info

[278], [81]

Org-23366

Drug Info

[35]

PD-157695

Drug Info

[35]

PD-158771

Drug Info

[35]

Dianicline+rimonabant

Drug Info

[303]

GMC-283

Drug Info

[35]

(+)-S-14297

Drug Info

[313]

Anti-D

Drug Info

[348]

CLR-151

Drug Info

[248]

ML321

Drug Info

[367]

S-(-)-sulpiride

Drug Info

[207], [233], [234]

[3H]N-methylspiperone

Drug Info

[392], [393]

[3H]spiperone

Drug Info

[394], [312]

Inhibitor

[+] 187 Inhibitor drugs

Aniracetam

Drug Info

[186]

Phenyltoloxamine

Drug Info

[224]

P2B-001

Drug Info

[243]

ROXINDOLE

Drug Info

[254]

TIOSPIRONE

Drug Info

[281]

MAZAPERTINE

Drug Info

[284]

PGX-200097

Drug Info

[296]

A-68930

Drug Info

[297]

A-80426

Drug Info

[298]

PD-128483

Drug Info

[308]

(+)-(1R,1'S)-berbamunine hydrochloride

Drug Info

[311]

(+)-(1R,1'S)-thaligrisine hydrochloride

Drug Info

[311]

(+)-BUTACLAMOL

Drug Info

[312]

(+/-)-nantenine

Drug Info

[314]

(-)-(1S,1'R)-O,O-dimethylgrisbine hydrochloride

Drug Info

[311]

(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile

Drug Info

[315]

(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine

Drug Info

[316]

(4-Quinolin-2-ylpiperazin-1-yl)acetic Acid

Drug Info

[317]

(5-Methoxy-chroman-3-yl)-dipropyl-amine

Drug Info

[318]

(R)-(+)-coclaurine

Drug Info

[319]

(R)-(-)-10-methyl-11-hydroxyaporphine

Drug Info

[320]

(R)-(-)-11-hydroxy-N-n-propylnoraporphine

Drug Info

[321]

(R)-(-)-2-methoxy-11-hydroxyaporphine

Drug Info

[321]

(R)-(-)-2-methoxy-N-npropylnorapomorphine

Drug Info

[321]

(R)-(-)-2-Methyl-apomorphine hydrochloride

Drug Info

[322]

(R)-(-)-2-Phenyl-apomorphine hydrochloride

Drug Info

[322]

(R)-(-)-N-ethyl-2-methoxy-11-hydroxynoraporphine

Drug Info

[321]

(R)-(-)-N-propyl-2-methoxy-11-hydroxynoraporphine

Drug Info

[321]

(S)-BULBOCAPNINE

Drug Info

[323]

(S)-secoantioquine hydrochloride

Drug Info

[311]

(S)APOMORPHINE

Drug Info

[324]

(S,R)-isotetrandrine hydrochloride

Drug Info

[311]

(S,R)-pseudoxandrine hydrochloride

Drug Info

[311]

(S,S)-oxandrine hydrochloride

Drug Info

[311]

1,2,3,7,12,12a-hexahydro-1-aza-pleiadene-5,6-diol

Drug Info

[323]

1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane

Drug Info

[325]

1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane

Drug Info

[325]

1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane

Drug Info

[325]

1,6-bis(4-m-tolylpiperazin-1-yl)hexane

Drug Info

[325]

1,6-bis(4-phenylpiperazin-1-yl)hexane

Drug Info

[325]

1-(3-Hydroxyphenyl)-4-propylpiperazine

Drug Info

[245]

1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine

Drug Info

[326]

1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one

Drug Info

[327]

1-(benzyloxy)-2-(2-phenylethyl)benzene

Drug Info

[328]

1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene

Drug Info

[328]

1-Aminomethyl-3-cyclohexyl-isochroman-5,6-diol

Drug Info

[329]

1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine

Drug Info

[330]

1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine

Drug Info

[330]

1-Benzyl-4-(3-hydroxyphenyl)piperidine

Drug Info

[245]

1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine

Drug Info

[330]

1-Benzyl-4-pyrrol-1-yl-piperidine

Drug Info

[330]

1-Benzyl-4-[3-(methylsulfonyl)phenyl]piperazine

Drug Info

[245]

1-Benzyl-4-[3-(methylsulfonyl)phenyl]piperidine

Drug Info

[245]

1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine

Drug Info

[331]

1-Methyl-1,2,3,4-tetrahydro-isoquinoline-6,7-diol

Drug Info

[332]

1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine

Drug Info

[333]

1-Propyl-3-m-tolyl-piperidine hydrochloride

Drug Info

[334]

1-Propyl-3-o-tolyl-piperidine hydrochloride

Drug Info

[334]

1-Propyl-3-p-tolyl-piperidine hydrochloride

Drug Info

[334]

1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene

Drug Info

[328]

1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine

Drug Info

[224]

1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine

Drug Info

[224]

2,3-Dihydro-1H-indol-5-ol

Drug Info

[332]

2-(4-Dipropylamino-cyclohexylidene)-malononitrile

Drug Info

[316]

2-methoxyapomorphine

Drug Info

[335]

2-Methyl-8-phenyl-1,2,3,4-tetrahydro-isoquinoline

Drug Info

[336]

2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine

Drug Info

[328]

2-{[R-(-)-Apomorphine-2'-oxy]ethoxy}-ethanol

Drug Info

[335]

3,8-dibromoboldine

Drug Info

[337]

3-(1-Propyl-pyrrolidin-3-yl)-phenol

Drug Info

[333]

3-(2,3-Dimethyl-phenyl)-1-propyl-piperidine

Drug Info

[338]

3-(2,3-Dimethyl-phenyl)-piperidine

Drug Info

[338]

3-(2,5-Dimethyl-phenyl)-1-propyl-piperidine

Drug Info

[338]

3-(2,6-Dimethyl-phenyl)-1-propyl-piperidine

Drug Info

[338]

3-(2-Benzylamino-ethoxy)-phenol

Drug Info

[339]

3-(3,4-Dimethyl-phenyl)-1-propyl-piperidine

Drug Info

[338]

3-(3,4-Dimethyl-phenyl)-piperidine

Drug Info

[338]

3-(3,5-Dimethyl-phenyl)-1-propyl-piperidine

Drug Info

[338]

3-(4-Benzyl-piperazin-1-yl)-phenol

Drug Info

[340]

3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one

Drug Info

[312]

3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole

Drug Info

[341]

3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole

Drug Info

[341]

3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole

Drug Info

[341]

3-(Octahydro-indolizin-8-yl)-phenol

Drug Info

[342]

3-(Octahydro-quinolizin-3-yl)-phenol

Drug Info

[342]

3-bromoboldine

Drug Info

[337]

3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol

Drug Info

[343]

3-Chloroboldine

Drug Info

[337]

3-Cyclohexyl-1-propyl-piperidine hydrochloride

Drug Info

[334]

3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol

Drug Info

[343]

3-Iodoboldine

Drug Info

[337]

3-Naphthalen-1-yl-1-propyl-pyrrolidine

Drug Info

[333]

3-Naphthalen-1-yl-pyrrolidine

Drug Info

[333]

3-Phenyl-1-propyl-piperidine hydrochloride

Drug Info

[334]

3-Phenyl-1-propyl-pyrrolidine

Drug Info

[333]

3-Phenyl-pyrrolidine

Drug Info

[333]

3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine

Drug Info

[328]

4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one

Drug Info

[339]

4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole

Drug Info

[340]

100

4-(4-Benzyl-piperazin-1-yl)-1H-indole

Drug Info

[340]

101

4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole

Drug Info

[340]

102

4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole

Drug Info

[340]

103

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[344]

104

4-Benzyl-1-chroman-2-ylmethyl-piperidine

Drug Info

[312]

105

4-Benzyl-1-chroman-3-ylmethyl-piperidine

Drug Info

[312]

106

4-Benzyl-1-indan-2-ylmethyl-piperidine

Drug Info

[312]

107

5-OH-DPAT

Drug Info

[345]

108

A-690344

Drug Info

[346]

109

A-706149

Drug Info

[347]

110

ANOLOBINE

Drug Info

[323]

111

ANONAINE

Drug Info

[323]

112

Azaperone

Drug Info

[349]

113

Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine

Drug Info

[339]

114

Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine

Drug Info

[339]

115

Bis-{[R-(-)-apomorphine-2-oxy]ethyl} ether

Drug Info

[335]

116

BOLDINE

Drug Info

[337]

117

BRL-25594

Drug Info

[350]

118

BRL-26175

Drug Info

[351]

119

CLEBOPRIDE

Drug Info

[350]

120

D-189

Drug Info

[352]

121

D-190

Drug Info

[352]

122

D-192

Drug Info

[352]

123

D-193

Drug Info

[352]

124

D-203

Drug Info

[352]

125

D-210

Drug Info

[352]

126

D-218

Drug Info

[352]

127

D-219

Drug Info

[352]

128

D-220

Drug Info

[352]

129

D-237

Drug Info

[353]

130

D-264

Drug Info

[354]

131

D-315

Drug Info

[355]

132

D-366

Drug Info

[345]

133

EPIDEPRIDE

Drug Info

[356]

134

Ethyl-(4,5,6,7-tetrahydro-2H-indazol-5-yl)-amine

Drug Info

[357]

135

ETICLOPRIDE

Drug Info

[358]

136

Etoloxamine

Drug Info

[224]

137

FLUANISONE

Drug Info

[359]

138

FLUMEZAPINE

Drug Info

[360]

139

FLUTROLINE

Drug Info

[361]

140

GLAUCINE

Drug Info

[323]

141

IBZM

Drug Info

[356]

142

IODOPRIDE

Drug Info

[356]

143

IODOSULPIRIDE

Drug Info

[356]

144

ISOCLOZAPINE

Drug Info

[362]

145

ISOLOXAPINE

Drug Info

[363]

146

L-741626

Drug Info

[364]

147

MCL-515

Drug Info

[366]

148

MCL-516

Drug Info

[366]

149

N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide

Drug Info

[365]

150

N-Ethyl-2-methylnorapomorphine hydrochloride

Drug Info

[369]

151

N-Ethyl-2-phenylnorapomorphine hydrochloride

Drug Info

[369]

152

N-Propyl-2-methylnorapomorphine hydrochloride

Drug Info

[369]

153

N-Propyl-2-phenylnorapomorphine hydrochloride

Drug Info

[369]

154

N-propylnorapomorphine

Drug Info

[370], [321]

155

NOR-ROEFRACTINE

Drug Info

[319]

156

OCTOCLOTHEPIN

Drug Info

[371]

157

PD-135111

Drug Info

[308]

158

PD-135146

Drug Info

[308]

159

PD-135188

Drug Info

[308]

160

PD-135222

Drug Info

[308]

161

PD-135385

Drug Info

[308]

162

PD-135478

Drug Info

[308]

163

PD-135540

Drug Info

[308]

164

PD-137789

Drug Info

[308]

165

PD-137821

Drug Info

[308]

166

PD-168077

Drug Info

[334]

167

PD-172938

Drug Info

[373]

168

PD-172939

Drug Info

[373]

169

PG-01037

Drug Info

[374]

170

Preclamol

Drug Info

[342]

171

Propyl-(4,5,6,7-tetrahydro-2H-indazol-5-yl)-amine

Drug Info

[357]

172

PUKATEINE

Drug Info

[323]

173

QUINPIROLE

Drug Info

[338]

174

Ro-21-7767

Drug Info

[376]

175

SB-258719

Drug Info

[377]

176

SB-271046

Drug Info

[378]

177

SCH-24518

Drug Info

[380]

178

SK&F-89626

Drug Info

[382]

179

SKF-89124A

Drug Info

[383]

180

SLV-314

Drug Info

[384]

181

SNAP-94847

Drug Info

[385]

182

STEPHOLIDINE

Drug Info

[386]

183

UH-232

Drug Info

[387]

184

UH-301

Drug Info

[388]

185

WAY-208466

Drug Info

[391]

186

[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine

Drug Info

[339]

187

[3H]7-OH-DPAT

Drug Info

[353]

Agonist

[+] 45 Agonist drugs

Apomorphine

Drug Info

[187]

Aripiprazole

Drug Info

[188]

Bromocriptine

Drug Info

[1], [191], [192]

Cabergoline

Drug Info

[193], [194]

Dihydroergotoxine

Drug Info

[31]

Dopamine

Drug Info

[200], [201]

Ephedrine

Drug Info

[39]

Ergonovine

Drug Info

[203]

Mephentermine

Drug Info

[208]

Mesoridazine

Drug Info

[209]

Metaraminol

Drug Info

[210]

Methamphetamine

Drug Info

[54]

Methyldopa

Drug Info

[211]

N-0923

Drug Info

[106]

Naphazoline

Drug Info

[215]

Nemonapride

Drug Info

[35]

Phenylephrine

Drug Info

[222], [223]

Quetiapine

Drug Info

[35], [182], [230]

Ziprasidone

Drug Info

[239]

CQA 206-291

Drug Info

[241]

Entacapone+levodopa+carbidopa

Drug Info

[242]

Sumanirole

Drug Info

[106]

JNJ-37822681

Drug Info

[251]

Pardoprunox

Drug Info

[75]

XP-21279

Drug Info

[258]

(-)-3PPP, Maryland

Drug Info

[35]

Carmoxirole

Drug Info

[261]

Lu-02-750

Drug Info

[262]

Fencamfamine

Drug Info

[270]

NOLOMIROLE HYDROCHLORIDE

Drug Info

[279], [2]

SAVOXEPIN MESYLATE

Drug Info

[287], [2]

AM-831

Drug Info

[289]

AMR-103

Drug Info

[299]

Y-20024

Drug Info

[310], [2]

LP-211

Drug Info

[365]

MLS1547

Drug Info

[368]

PD 128907

Drug Info

[372]

PF-03800130

Drug Info

[248]

piribedil

Drug Info

[375]

Rotigitine

Drug Info

[25]

Uinagolide

Drug Info

[389]

UNC0006

Drug Info

[390]

UNC9975

Drug Info

[390]

UNC9994

Drug Info

[390]

WS-50030

Drug Info

[248]

Modulator

[+] 57 Modulator drugs

Cariprazine

Drug Info

[28]

Denopamine

Drug Info

[14]

Docarpamine

Drug Info

[14]

Levodopa

Drug Info

[45]

Levomepromazine

Drug Info

[205]

Lurasidone hydrochloride

Drug Info

[47], [48]

OPC-34712

Drug Info

[216], [217]

Perazine

Drug Info

[218], [2]

Pergolide

Drug Info

[205]

Piperacetazine

Drug Info

[205]

Pramipexole

Drug Info

[205]

Ropinirole

Drug Info

[205]

Bis(olanzapine) pamoate monohydrate

Drug Info

[2]

Lu AF35700

Drug Info

[101]

Pridopidine

Drug Info

[244], [245]

RBP-7000

Drug Info

[246]

Zicronapine

Drug Info

[247]

BIM23A760

Drug Info

[112]

CGS-15873A

Drug Info

[249], [2]

CLR-3001

Drug Info

[250]

Mazapertine succinate

Drug Info

[252]

Ocaperidone

Drug Info

[119]

PD-143188

Drug Info

[253]

SDZ-MAR-327

Drug Info

[257]

Abaperidone

Drug Info

[259]

ATI-9242

Drug Info

[260]

Lu-AE04621

Drug Info

[263]

SSR-181507

Drug Info

[265]

YKP-1358

Drug Info

[267]

Bifeprunox

Drug Info

[277]

Sibenadet

Drug Info

[280]

BAM-1110

Drug Info

[282]

Declopramide

Drug Info

[283]

Naxagolide

Drug Info

[285]

PF-217830

Drug Info

[252]

Romergoline

Drug Info

[286]

SLV-310

Drug Info

[288]

DU-29894

Drug Info

[290]

Ordopidine

Drug Info

[291]

S-18327

Drug Info

[292]

SDZ-GLC-756

Drug Info

[293]

SLV-313

Drug Info

[294]

F-15063

Drug Info

[295]

S32504

Drug Info

[164]

BIMG80

Drug Info

[300]

CGP-25454A

Drug Info

[301]

CP-903397

Drug Info

[302]

E-2040

Drug Info

[304]

Etrabamine

Drug Info

[305]

LY-243062

Drug Info

[306]

NGD-93-1

Drug Info

[307]

NNC-22-0031

Drug Info

[177]

Org-10490

Drug Info

[205]

PNU-96391A

Drug Info

[179]

RWJ-25730

Drug Info

[309]

SDZ-208911

Drug Info

[381], [2]

SEL-73

Drug Info

[248]

Binder

[+] 5 Binder drugs

Droperidol

Drug Info

[202]

Molindone

Drug Info

[213], [214]

SKL-10406

Drug Info

[264]

Y-931

Drug Info

[35]

ZD-3638

Drug Info

[35]

Stimulator

[+] 1 Stimulator drugs

Pseudoephedrine

Drug Info

[228], [229]

Ligand

[+] 10 Ligand drugs

Aryl piperazine derivative 1

Drug Info

[137]

Benzo[d]oxazol-2(3H)-one derivative 1

Drug Info

[268]

Benzo[d]oxazol-2(3H)-one derivative 2

Drug Info

[268]

Benzo[d]oxazol-2(3H)-one derivative 3

Drug Info

[268]

PMID29334795-Compound-62

Drug Info

[268]

PMID29334795-Compound-66

Drug Info

[268]

PMID29334795-Compound-67

Drug Info

[268]

PMID30124346-Compound-13TABLE4

Drug Info

[137]

PMID30124346-Compound-34TABLE4

Drug Info

[137]

PMID30124346-Compound-60TABLE5

Drug Info

[137]

Modulator (allosteric modulator)

[+] 1 Modulator (allosteric modulator) drugs

SB269652

Drug Info

[379]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Drug Binding Sites of Target

Top

Ligand Name: Bromocriptine

Ligand Info

Structure Description

Structure of a D2 dopamine receptor-G-protein complex in a lipid membrane

PDB:6VMS

Method

Electron microscopy

Resolution

3.80 Å

Mutation

[395]

PDB Sequence

PHYNYYATLL

⁴¹

TLLIAVIVFG

⁵¹

NVLVCMAVSR

⁶¹

EKALQTTTNY

⁷¹

LIVSLAVADL

⁸¹

LVATLVMPWV

⁹¹

VYLEVVGEWK

¹⁰¹

FSRIHCDIFV

¹¹¹

TLDVMMCTAS

¹²¹

ILNLCAISID

¹³¹

RYTAVAMPML

¹⁴¹

YNTRYSSKRR

¹⁵¹

VTVMISIVWV

¹⁶¹

LSFTISCPLL

¹⁷¹

FGLNNADQNE

¹⁸¹

CIIANPAFVV

¹⁹¹

YSSIVSFYVP

²⁰¹

FIVILLVYIK

²¹¹

IYIVLRRRRK

²²¹

LVNTNRKLSQ

³⁶⁵

QKEKKATQLL

³⁷⁵

AIYLGLFIIC

³⁸⁵

WLPFFITHIL

³⁹⁵

NIHCDCNIPP

⁴⁰⁵

VLYSAFTWLG

⁴¹⁵

YVNSAINPII

⁴²⁵

YTTFNIEFRK

⁴³⁵

AFLKILHC

Residue

Distance (Å)

LEU94

4.374

PHE110

3.541

VAL111

3.516

ASP114

2.759

VAL115

3.914

CYS118

3.425

THR119

3.464

ILE122

3.417

CYS182

3.298

ILE183

3.790

ILE184

3.505

PHE189

4.963

VAL190

3.623

Residue

Distance (Å)

SER193

3.901

SER194

4.758

SER197

3.563

TRP386

3.715

PHE389

3.533

PHE390

3.570

HIS393

3.662

PRO405

4.367

TYR408

3.845

SER409

4.098

THR412

3.308

TYR416

3.780

Ligand Name: Risperidone

Ligand Info

Structure Description

Structure of the D2 Dopamine Receptor Bound to the Atypical Antipsychotic Drug Risperidone

PDB:6CM4

Method

X-ray diffraction

Resolution

2.87 Å

Mutation

[396]

PDB Sequence

NYYATLLTLL

⁴⁴

IAVIVFGNVL

⁵⁴

VCMAVSREKA

⁶⁴

LQTTTNYLIV

⁷⁴

SLAVADLLVA

⁸⁴

TLVMPWVVYL

⁹⁴

EVVGEWKFSR

¹⁰⁴

IHCDIFVTLD

¹¹⁴

VMMCTASALN

¹²⁴

LCAISIDRYT

¹³⁴

AVAMPTRYSS

¹⁴⁸

KRRVTVMISI

¹⁵⁸

VWVLSFTISC

¹⁶⁸

PLLFGLNNAD

¹⁷⁸

QNECIIANPA

¹⁸⁸

FVVYSSIVSF

¹⁹⁸

YVPFIVTLLV

²⁰⁸

YIKIYIVLRR

²¹⁸

RRKRNIFEML

¹⁰⁰⁷

RIDEGLRLKI

¹⁰¹⁷

YKDTEGYYTI

¹⁰²⁷

GIGHLLTKSP

¹⁰³⁷

SLNAAKSELD

¹⁰⁴⁷

KAIGRNTNGV

¹⁰⁵⁷

ITKDEAEKLF

¹⁰⁶⁷

NQDVDAAVRG

¹⁰⁷⁷

ILRNAKLKPV

¹⁰⁸⁷

YDSLDAVRRA

¹⁰⁹⁷

ALINMVFQMG

¹¹⁰⁷

ETGVAGFTNS

¹¹¹⁷

LRMLQQKRWD

¹¹²⁷

EAAVNLAKSR

¹¹³⁷

WYNQTPNRAK

¹¹⁴⁷

RVITTFRTGT

¹¹⁵⁷

WDAYSQQKEK

³⁶⁹

KATQMAAIVA

³⁷⁹

GVFIICWLPF

³⁸⁹

FITHILNIHC

³⁹⁹

DCNIPPVLYS

⁴⁰⁹

AFTWLGYVNS

⁴¹⁹

AVNPIIYTTF

⁴²⁹

NIEFRKAFLK

⁴³⁹

ILH

Residue

Distance (Å)

VAL91

4.442

LEU94

4.082

TRP100

3.497

PHE110

3.744

ASP114

2.694

VAL115

3.803

CYS118

3.334

THR119

3.727

ALA122

3.306

ILE184

4.478

PHE189

4.459

SER193

3.996

Residue

Distance (Å)

SER197

3.317

PHE198

3.715

PHE382

3.440

TRP386

3.363

PHE389

3.295

PHE390

3.556

HIS393

4.830

TYR408

3.746

SER409

4.022

THR412

3.673

TYR416

3.411

Click to View More Binding Site Information of This Target with Different Ligands

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Human Pathway Affiliation Biological Network Descriptors

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Human Pathway Affiliation

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 2T34 (OR2T34)	PF13853	26.667 (40/150)	1.69E-08
Olfactory receptor 2T3 (OR2T3)	PF13853	26.667 (40/150)	2.45E-08
Olfactory receptor 4K5 (OR4K5)	PF13853	27.215 (43/158)	1.19E-06
Olfactory receptor 9A1 (OR9A1P)	PF13853	29.457 (38/129)	1.57E-06
Olfactory receptor 2L2 (OR2L2)	PF13853	28.462 (37/130)	2.44E-06
Olfactory receptor 9A2 (OR9A2)	PF13853	27.083 (39/144)	6.88E-06
Olfactory receptor 4K3 (OR4K3)	PF13853	23.404 (55/235)	1.12E-05
Olfactory receptor 10A6 (OR10A6)	PF13853	22.530 (57/253)	2.83E-05
Olfactory receptor 4D10 (OR4D10)	PF13853	26.087 (30/115)	3.06E-05
Olfactory receptor 2L5 (OR2L5)	PF13853	26.357 (34/129)	6.15E-05
Olfactory receptor 1D2 (OR1D2)	PF13853	28.906 (37/128)	6.78E-05
Olfactory receptor 1D4 (OR1D4)	PF13853	25.325 (39/154)	1.09E-04
Olfactory receptor 13A1 (OR13A1)	PF13853	23.188 (32/138)	1.68E-04
Olfactory receptor 9A4 (OR9A4)	PF13853	24.306 (35/144)	1.89E-04
Olfactory receptor 14J1 (OR14J1)	PF13853	24.762 (26/105)	2.04E-04
Olfactory receptor 4D11 (OR4D11)	PF13853	26.724 (31/116)	2.30E-04
Olfactory receptor 2AG1 (OR2AG1)	PF13853	28.455 (35/123)	2.32E-04
Olfactory receptor 1D5 (OR1D5)	PF13853	25.325 (39/154)	2.64E-04
Olfactory receptor 52Z1P (OR52Z1P)	PF13853	28.906 (37/128)	3.36E-04
Olfactory receptor 10W1 (OR10W1)	PF13853	23.529 (24/102)	3.59E-04
Olfactory receptor 2M7 (OR2M7)	PF13853	21.053 (32/152)	4.91E-04
Olfactory receptor 1L1 (OR1L1)	PF13853	28.395 (46/162)	7.45E-04
Olfactory receptor 2AG2 (OR2AG2)	PF13853	29.008 (38/131)	7.93E-04
Olfactory receptor 14A16 (OR14A16)	PF13853	26.446 (32/121)	1.00E-03
Olfactory receptor 2L3 (OR2L3)	PF13853	24.031 (31/129)	1.00E-03
Olfactory receptor 5P2 (OR5P2)	PF13853	24.113 (34/141)	1.00E-03
Olfactory receptor 2F1 (OR2F1)	PF13853	22.581 (56/248)	1.00E-03
Olfactory receptor 11A1 (OR11A1)	PF13853	24.551 (41/167)	2.00E-03
Olfactory receptor 2L8 (OR2L8)	PF13853	25.424 (30/118)	2.00E-03
Olfactory receptor 2F2 (OR2F2)	PF13853	22.400 (56/250)	2.00E-03
Olfactory receptor 8D2 (OR8D2)	PF13853	26.271 (31/118)	2.00E-03
Olfactory receptor 2AT4 (OR2AT4)	PF13853	23.529 (28/119)	2.00E-03
Olfactory receptor 4F6 (OR4F6)	PF13853	24.242 (40/165)	3.00E-03
Olfactory receptor 5AS1 (OR5AS1)	PF13853	28.846 (30/104)	3.00E-03
Putative olfactory receptor 2W6 (OR2W6P)	PF13853	22.302 (31/139)	3.00E-03
Olfactory receptor 2AJ1 (OR2AJ1)	PF13853	27.473 (25/91)	4.00E-03
Olfactory receptor 10C1 (OR10C1)	PF13853	23.438 (30/128)	5.00E-03
Olfactory receptor 4D2 (OR4D2)	PF13853	23.030 (38/165)	5.00E-03
Olfactory receptor 2D3 (OR2D3)	PF13853	32.653 (32/98)	5.00E-03
Olfactory receptor 2V1 (OR2V1)	PF13853	25.806 (32/124)	5.00E-03
Olfactory receptor 2M3 (OR2M3)	PF13853	21.642 (29/134)	5.00E-03
Olfactory receptor 5M9 (OR5M9)	PF13853	22.430 (48/214)	5.00E-03
Olfactory receptor 4K13 (OR4K13)	PF13853	26.126 (29/111)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins

KEGG Pathway	Pathway ID	Affiliated Target
Rap1 signaling pathway	hsa04015	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
cAMP signaling pathway	hsa04024	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy
Gap junction	hsa04540	Affiliated Target
Class: Cellular Processes => Cellular community - eukaryotes	Pathway Hierarchy
Dopaminergic synapse	hsa04728	Affiliated Target
Class: Organismal Systems => Nervous system	Pathway Hierarchy

Degree	10	Degree centrality	1.07E-03	Betweenness centrality	4.80E-04
Closeness centrality	2.13E-01	Radiality	1.37E+01	Clustering coefficient	4.44E-02
Neighborhood connectivity	1.42E+01	Topological coefficient	1.22E-01	Eccentricity	12
Download	Click to Download the Full PPI Network of This Target

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 8 KEGG Pathways

Rap1 signaling pathway

cAMP signaling pathway

Neuroactive ligand-receptor interaction

Gap junction

Dopaminergic synapse

Parkinson's disease

Cocaine addiction

Alcoholism

Panther Pathway

[+] 4 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway

Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway

Dopamine receptor mediated signaling pathway

Nicotine pharmacodynamics pathway

Reactome

[+] 2 Reactome Pathways

Dopamine receptors

G alpha (i) signalling events

WikiPathways

[+] 7 WikiPathways

Hypothetical Network for Drug Addiction

Monoamine GPCRs

GPCRs, Class A Rhodopsin-like

Genes and (Common) Pathways Underlying Drug Addiction

GPCR ligand binding

GPCR downstream signaling

Nicotine Activity on Dopaminergic Neurons

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Silymarin BIO-C, an extract from Silybum marianum fruits, induces hyperprolactinemia in intact female rats. Phytomedicine. 2009 Sep;16(9):839-44.

REF 2

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 3

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7306).

REF 4

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012753.

REF 5

REF 6

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080439.

REF 7

REF 8

Olanzapine: an updated review of its use in the management of schizophrenia. Drugs. 2001;61(1):111-61.

REF 9

Sustained pain relief with dihydroergotamine in migraine is potentially due to persistent binding to 5-HT1B and 5-HT1D receptors. . The Journal of Headache and Pain 201314(Suppl 1):P75.

REF 10

REF 11

Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis. Clin Neuropharmacol. 2006 Mar-Apr;29(2):80-6.

REF 12

REF 13

Drug information of Fluspirilene, 2008. eduDrugs.

REF 14

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 15

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019

REF 16

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012254.

REF 17

REF 18

REF 19

Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.

REF 20

REF 21

ClinicalTrials.gov (NCT02339064) Infusion of Apomorphine: Long-term Safety Study. U.S. National Institutes of Health.

REF 22

REF 23

Electrophysiological studies in the rat brain on the basis for aripiprazole augmentation of antidepressants in major depressive disorder. Psychopharmacology (Berl). 2009 Oct;206(2):335-44.

REF 24

REF 25

Novel pharmacological targets for the treatment of Parkinson's disease. Nat Rev Drug Discov. 2006 Oct;5(10):845-54.

REF 26

REF 27

REF 28

Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.

REF 29

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016149.

REF 30

REF 31

Pharmacologic management of Alzheimer disease, Part II: Antioxidants, antihypertensives, and ergoloid derivatives. Ann Pharmacother. 1999 Feb;33(2):188-97.

REF 32

REF 33

A systematic review of the efficacy of domperidone for the treatment of diabetic gastroparesis. Clin Gastroenterol Hepatol. 2008 Jul;6(7):726-33.

REF 34

REF 35

The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.

REF 36

REF 37

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 072123.

REF 38

REF 39

The effect of alpha-2 adrenergic agonists on memory and cognitive flexibility. Cogn Behav Neurol. 2006 Dec;19(4):204-7.

REF 40

REF 41

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006035.

REF 42

REF 43

REF 44

Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.

REF 45

REF 46

REF 47

Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.

REF 48

Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81.

REF 49

New drugs for type 2 diabetes mellitus: what is their place in therapy Drugs. 2008;68(15):2131-62.

REF 50

REF 51

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016774.

REF 52

REF 53

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 080722.

REF 54

Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.

REF 55

REF 56

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070075.

REF 57

REF 58

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070184.

REF 59

REF 60

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017111.

REF 61

2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.

REF 62

Rotigotine: a novel dopamine agonist for the transdermal treatment of Parkinson's disease. Drugs Today (Barc). 2006 Jan;42(1):21-8.

REF 63

REF 64

REF 65

ClinicalTrials.gov (NCT01397786) Safety and Tolerability Study of Oral OPC-34712 as Maintenance Treatment in Adults With Schizophrenia. U.S. National Institutes of Health.

REF 66

REF 67

REF 68

Methamphetamine Addiction and Abuse - Perphenazine.

REF 69

REF 70

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040235.

REF 71

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019494)

REF 72

REF 73

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017473.

REF 74

REF 75

Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.

REF 76

REF 77

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040058.

REF 78

REF 79

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075153.

REF 80

REF 81

How many modes of action should an antibiotic have Curr Opin Pharmacol. 2008 Oct;8(5):564-73.

REF 82

REF 83

Emerging anxiolytics. Expert Opin Emerg Drugs. 2007 Nov;12(4):541-54.

REF 84

REF 85

Update on ropinirole in the treatment of Parkinson's disease. Neuropsychiatr Dis Treat. 2009;5:33-6.

REF 86

REF 87

Persistence and compliance to antidepressant treatment in patients with depression: a chart review. BMC Psychiatry. 2009 Jun 16;9:38.

REF 88

REF 89

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 088001.

REF 90

REF 91

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070600.

REF 92

REF 93

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006403.

REF 94

REF 95

REF 96

Drug information of Zuclopenthixol, 2008. eduDrugs.

REF 97

ClinicalTrials.gov (NCT05227209) A 12-Month Open-label Extension Study to Evaluate the Long-term Safety, Tolerability, and Effectiveness of SEP-4199 Controlled Release (CR) for the Treatment of Major Depressive Episode Associated With Bipolar I Disorder (Bipolar I Depression). U.S.National Institutes of Health.

REF 98

REF 99

CQA 206-291: a novel dopamine agonist in the treatment of Parkinson's disease. Clin Neuropharmacol. 1990 Aug;13(4):303-11.

REF 100

Optimizing levodopa therapy for Parkinson's disease with levodopa/carbidopa/entacapone: implications from a clinical and patient perspective. Neuropsychiatr Dis Treat. 2008 February; 4(1): 39-47.

REF 101

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 102

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 103

ClinicalTrials.gov (NCT00665223) A Study of Treatment With ACR16 in Patients With Huntington's Disease. U.S. National Institutes of Health.

REF 104

ClinicalTrials.gov (NCT02109562) Randomized, Double-blind, Placebo Controlled, Multi-center and Tolerability of RBP-7000 in Schizophrenia Patients. U.S. National Institutes of Health.

REF 105

REF 106

Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.

REF 107

ClinicalTrials.gov (NCT01295372) Safety and Efficacy of Zicronapine in Patients With Schizophrenia. U.S. National Institutes of Health.

REF 108

ClinicalTrials.gov (NCT04335357) TBR-760 in Adult Patients With Non-Functioning Pituitary Adenomas. U.S. National Institutes of Health.

REF 109

ClinicalTrials.gov (NCT03544229) A Study to Evaluate the Efficacy and Safety of TAK-906 in Adult Participants With Symptomatic Idiopathic or Diabetic Gastroparesis. U.S. National Institutes of Health.

REF 110

ClinicalTrials.gov (NCT03543410) A Clinical Study to Test the Effectiveness of an Investigational Drug to Treat People That Have Major Depressive Episodes When They Have Bipolar 1 Depression. U.S. National Institutes of Health.

REF 111

ClinicalTrials.gov (NCT01857232) Dose-finding Study of APD403 to Prevent Nausea and Vomiting After Chemotherapy. U.S. National Institutes of Health.

REF 112

BIM-23A760, a chimeric molecule directed towards somatostatin and dopamine receptors, vs universal somatostatin receptors ligands in GH-secreting pituitary adenomas partial responders to octreotide. J Endocrinol Invest. 2005;28(11 Suppl International):21-7.

REF 113

Emerging drugs for acromegaly. Expert Opin Emerg Drugs. 2008 Jun;13(2):273-93.

REF 114

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001412)

REF 115

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032468)

REF 116

ClinicalTrials.gov (NCT00728195) An Efficacy and Safety Study of 3 Fixed Doses of JNJ-37822681 in Participants With Schizophrenia. U.S. National Institutes of Health.

REF 117

Orally active benzamide antipsychotic agents with affinity for dopamine D2, serotonin 5-HT1A, and adrenergic alpha1 receptors. J Med Chem. 1998 Jun 4;41(12):1997-2009.

REF 118

REF 119

Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59.

REF 120

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 121

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005971)

REF 122

REF 123

Roxindole: psychopharmacological profile of a dopamine D2 autoreceptor agonist. J Pharmacol Exp Ther. 1996 Jan;276(1):41-8.

REF 124

ClinicalTrials.gov (NCT01490086) RP5063 in Subjects With Schizophrenia or Schizoaffective Disorder. U.S. National Institutes of Health.

REF 125

Positron emission tomographic analysis of central dopamine D1 receptor binding in normal subjects treated with the atypical neuroleptic, SDZ MAR 327. Int J Mol Med. 1998 Jan;1(1):243-7.

REF 126

ClinicalTrials.gov (NCT01171313) A Efficacy, Safety and Pharmacokinetic Study of XP21279 and Sinemet in Parkinson's Disease Subjects. U.S. National Institutes of Health.

REF 127

ClinicalTrials.gov (NCT04541082) Phase I Study of Oral ONC206 in Recurrent and Rare Primary Central Nervous System Neoplasms. U.S. National Institutes of Health.

REF 128

ClinicalTrials.gov (NCT04291859) Interventional, Open-label, Exploratory Study, Investigating the Safety, Tolerability, Pharmacokinetics, and Efficacy of Lu AF28996 in Patients With Parkinson's Disease. U.S.National Institutes of Health.

REF 129

Pharmacologic properties of (-)-3PPP (preclamol) in man. J Neural Transm Gen Sect. 1992;88(3):165-75.

REF 130

1192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42.

REF 131

Small Molecule Therapeutics for Schizophrenia, Sylvain Celanire. Page(30).

REF 132

Pharmacokinetics and first clinical experiences with an antihypertensive dopamine (DA2) agonist. Eur Heart J. 1992 Sep;13 Suppl D:121-8.

REF 133

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031195)

REF 134

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031909)

REF 135

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032727)

REF 136

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000698)

REF 137

5-HT1A receptor ligands and their therapeutic applications: review of new patents.Expert Opin Ther Pat. 2018 Sep;28(9):679-689.

REF 138

mGlu5 negative allosteric modulators: a patent review (2013 - 2016).Expert Opin Ther Pat. 2017 Jun;27(6):691-706.

REF 139

Caspase inhibitors: a review of recently patented compounds (2013-2015).Expert Opin Ther Pat. 2018 Jan;28(1):47-59.

REF 140

Drug information of Fencamfamine, 2008. eduDrugs.

REF 141

REF 142

Behavioral responses of dopamine beta-hydroxylase knockout mice to modafinil suggest a dual noradrenergic-dopaminergic mechanism of action. Pharmacol Biochem Behav. 2008 Dec;91(2):217-22.

REF 143

REF 144

Pharmacology of the atypical antipsychotic remoxipride, a dopamine D2 receptor antagonist. CNS Drug Rev. 2001 Fall;7(3):265-82.

REF 145

REF 146

Sertindole: efficacy and safety in schizophrenia. Expert Opin Pharmacother. 2006 Sep;7(13):1825-34.

REF 147

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015146)

REF 148

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003364)

REF 149

Anti-obesity drugs and neural circuits of feeding. Trends Pharmacol Sci. 2008 Apr;29(4):208-17.

REF 150

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002585)

REF 151

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005232)

REF 152

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007055)

REF 153

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002657)

REF 154

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025560)

REF 155

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001388)

REF 156

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000647)

REF 157

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016551)

REF 158

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001422)

REF 159

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025217)

REF 160

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009651)

REF 161

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008736)

REF 162

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026348)

REF 163

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024498)

REF 164

S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: II. Actions in rodent, primate, and cellular models of antiparkinsonian activity ... J Pharmacol Exp Ther. 2004 Jun;309(3):921-35.

REF 165

Pharmacokinetics, Pharmacodynamics and Tolerance of SLV 307 After Single Oral Administration in Healthy Male Volunteers. Clinical Pharmacology &#38 Therapeutics. 02/1999; 65(2).

REF 166

REF 167

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002423)

REF 168

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025731)

REF 169

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006596)

REF 170

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004095)

REF 171

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025558)

REF 172

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027143)

REF 173

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)

REF 174

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003368)

REF 175

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005079)

REF 176

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002902)

REF 177

NNC-19-1228 and NNC 22-0031, novel neuroleptics with a "mesolimbic-selective" behavioral profile. Psychopharmacology (Berl). 1997 Jan;129(2):168-78.

REF 178

ORG 10490: A new antipsychotic drug with 5-HT2 and DA antagonistic properties. ScienceDirect, Volume 6, Issue 2, January 1992, Pages 111.

REF 179

The dopamine stabilizer (-)-OSU6162 occupies a subpopulation of striatal dopamine D2/D3 receptors: an [(11)C]raclopride PET study in healthy human subjects. Neuropsychopharmacology. 2015 Jan;40(2):472-9.

REF 180

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001430)

REF 181

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001374)

REF 182

Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38.

REF 183

Specific therapeutic actions of acetophenazine, perphenazine, and benzquinamide in newly admitted schizophrenic patients. Clin Pharmacol Ther. 1967 Mar-Apr;8(2):249-55.

REF 184

Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia. CNS Drugs. 2006;20(5):389-409.

REF 185

Amisulpride: a review of its use in the management of schizophrenia. CNS Drugs. 2004;18(13):933-56.

REF 186

Anxiolytic effects of aniracetam in three different mouse models of anxiety and the underlying mechanism. Eur J Pharmacol. 2001 May 18;420(1):33-43.

REF 187

Dopamine D(2/3) receptor occupancy of apomorphine in the nonhuman primate brain--a comparative PET study with [11C]raclopride and [11C]MNPA. Synapse. 2009 May;63(5):378-89.

REF 188

Aripiprazole acts as a selective dopamine D2 receptor partial agonist. Expert Opin Investig Drugs. 2007 Jun;16(6):771-5.

REF 189

Determination of bevantolol in human plasma by high performance liquid chromatography using solid phase extraction technique. Arch Pharm Res. 2007 Jul;30(7):890-7.

REF 190

Different changes of plasma membrane beta-adrenoceptors in rat heart after chronic administration of propranolol, atenolol and bevantolol. Life Sci. 2007 Jul 12;81(5):399-404.

REF 191

Striatal dopamine predicts outcome-specific reversal learning and its sensitivity to dopaminergic drug administration. J Neurosci. 2009 Feb 4;29(5):1538-43.

REF 192

The behavioral toxicity of bromocriptine in patients with psychiatric illness. J Clin Psychopharmacol. 1989 Dec;9(6):417-22.

REF 193

Role of D1 and D2 receptors in the regulation of voluntary movements. Bull Exp Biol Med. 2008 Jul;146(1):14-7.

REF 194

Protection against paraquat and A53T alpha-synuclein toxicity by cabergoline is partially mediated by dopamine receptors. J Neurol Sci. 2009 Mar 15;278(1-2):44-53.

REF 195

Comparison of dosage ranges of carphenazine and trifluoperazine in elderly chronic schizophrenics. Dis Nerv Syst. 1968 Oct;29(10):695-7.

REF 196

Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42.

REF 197

Effect of ibopamine on aqueous humor production in normotensive humans. Invest Ophthalmol Vis Sci. 2003 Nov;44(11):4853-8.

REF 198

Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.

REF 199

The significance of disordered gastric emptying. Z Gastroenterol. 1986 Sep;24 Suppl 2:45-54.

REF 200

The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.

REF 201

Polymorphisms in dopamine receptor DRD1 and DRD2 genes and psychopathological and extrapyramidal symptoms in patients on long-term antipsychotic treatment. Am J Med Genet B Neuropsychiatr Genet. 2007Sep 5;144B(6):809-15.

REF 202

Alpha-adrenergic blockade: a possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo. Life Sci. 2003 Jan 24;72(10):1093-102.

REF 203

Agonist profile of ergometrine (ergonovine) on a population of postsynaptic alpha-adrenoceptors. J Pharm Pharmacol. 1988 Feb;40(2):137-9.

REF 204

Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.

REF 205

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 206

Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain. Biochem Pharmacol. 1985 Jul 1;34(13):2251-9.

REF 207

The effects of antipsychotic drugs on Fos protein expression in the prefrontal cortex: cellular localization and pharmacological characterization. Neuroscience. 1996 Jan;70(2):377-89.

REF 208

Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor. Am Heart J. 1976 Nov;92(5):661-4.

REF 209

Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as... J Pharmacol Exp Ther. 2005 Dec;315(3):1278-87.

REF 210

Alpha1-adrenoceptor stimulation enhances experimental gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats. Int J Cancer. 1998 Jul 29;77(3):467-9.

REF 211

Centrally acting antihypertensive agents: an update. J Clin Hypertens (Greenwich). 2007 May;9(5):399-405.

REF 212

Mechanisms for metoclopramide-mediated sensitization and haloperidol-induced catalepsy in rats. Eur J Pharmacol. 2008 Jun 10;587(1-3):181-6.

REF 213

Molindone for schizophrenia and severe mental illness. Cochrane Database Syst Rev. 2007 Jan 24;(1):CD002083.

REF 214

Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol Psychiatry. 1998 Mar;3(2):123-34.

REF 215

Decongestants in treatment of nasal obstruction. Otolaryngol Pol. 1999;53(3):347-52.

REF 216

Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.

REF 217

Brexpiprazole: First Global Approval.Drugs.2015 Sep;75(14):1687-97.

REF 218

Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.

REF 219

CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.

REF 220

A cross-validation study on the relationship between central D2 receptor occupancy and serum perphenazine concentration. Psychopharmacology (Berl). 2004 Sep;175(2):148-53.

REF 221

Nesfatin-1 exerts cardiovascular actions in brain: possible interaction with the central melanocortin system. Am J Physiol Regul Integr Comp Physiol. 2009 Aug;297(2):R330-6.

REF 222

MMP-2 induced vein relaxation via inhibition of [Ca2+]e-dependent mechanisms of venous smooth muscle contraction. Role of RGD peptides. J Surg Res. 2010 Apr;159(2):755-64.

REF 223

Intracellular Ca2+ and adrenergic responsiveness of cardiac myocytes in streptozotocin-induced diabetes. Clin Exp Pharmacol Physiol. 1999 Apr;26(4):347-53.

REF 224

Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8.

REF 225

[The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.

REF 226

In vitro and in vivo characteristics of prochlorperazine oral disintegrating film. Int J Pharm. 2009 Feb 23;368(1-2):98-102.

REF 227

Tardive dyskinesia as a result of long-term prochlorperazine use. South Med J. 1996 Oct;89(10):989-91.

REF 228

Cetirizine/pseudoephedrine. Drugs. 2001;61(15):2231-40; discussion 2241-2.

REF 229

Drugs for cough and cold symptoms in hypertensive patients. Am Fam Physician. 1985 Mar;31(3):183-7.

REF 230

Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.

REF 231

Randomized clinical comparison of perospirone and risperidone in patients with schizophrenia: Kansai Psychiatric Multicenter Study. Psychiatry Clin Neurosci. 2009 Jun;63(3):322-8.

REF 232

Upcoming agents for the treatment of schizophrenia: mechanism of action, efficacy and tolerability. Drugs. 2008;68(16):2269-92.

REF 233

The treatment of Tourette's syndrome: current opinions. Expert Opin Pharmacother. 2002 Jul;3(7):899-914.

REF 234

D(2) dopamine receptors enable delta(9)-tetrahydrocannabinol induced memory impairment and reduction of hippocampal extracellular acetylcholine concentration. Br J Pharmacol. 2000 Jul;130(6):1201-10.

REF 235

Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4.

REF 236

Models of drug treatment in the attention deficit disorder with hyperactivity. Rev Neurol. 2002 Feb;34 Suppl 1:S98-S106.

REF 237

Dopaminergic stimulation of cAMP accumulation in cultured rat mesangial cells. Am J Physiol. 1987 Aug;253(2 Pt 2):H358-64.

REF 238

Comparative effects of tolazoline and nitroprusside on human isolated radial artery. Ann Thorac Surg. 2006 Jan;81(1):125-31.

REF 239

Striatal and extrastriatal D2/D3-receptor-binding properties of ziprasidone: a positron emission tomography study with [18F]Fallypride and [11C]raclopride (D2/D3-receptor occupancy of ziprasidone). JClin Psychopharmacol. 2008 Dec;28(6):608-17.

REF 240

An ethopharmacological assessment of the effects of zuclopenthixol on agonistic interactions in male mice. Methods Find Exp Clin Pharmacol. 1999 Jan-Feb;21(1):11-5.

REF 241

The antiparkinsonian activity of CQA 206-291, a new D2 dopamine receptor agonist. Clin Neuropharmacol. 1989 Feb;12(1):55-9.

REF 242

Emerging drugs for restless legs syndrome. Expert Opin Emerg Drugs. 2005 Aug;10(3):537-52.

REF 243

Pharmacology of pramipexole, a dopamine D3-preferring agonist useful in treating Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):141-51.

REF 244

Efficacy and safety of the dopaminergic stabilizer Pridopidine (ACR16) in patients with Huntington's disease. Clin Neuropharmacol. 2010 Sep-Oct;33(5):260-4.

REF 245

Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabi... J Med Chem. 2010 Mar 25;53(6):2510-20.

REF 246

Population pharmacokinetics and prediction of dopamine D2 receptor occupancy after multiple doses of RBP-7000, a new sustained-release formulation of risperidone, in schizophrenia patients on stable oral risperidone treatment. Clin Pharmacokinet. 2014 Jun;53(6):533-43.

REF 247

Clinical pipeline report, company report or official report of Lundbeck.

REF 248

REF 249

Biochemical and pharmacological characterization of the putative dopamine autoreceptor agonist benzopyranopyridine, CGS 15873A. Article first published online: 5 OCT 2004.

REF 250

Clinical pipeline report, company report or official report of Clera Inc.

REF 251

Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D receptor occupancy. Clin Pharmacokinet. 2013 Nov;52(11):1005-15.

REF 252

Dual ligands targeting dopamine D2 and serotonin 5-HT1A receptors as new antipsychotical or anti-Parkinsonian agents.Curr Med Chem.2014;21(4):437-57.

REF 253

Anxiolytic effects of dopamine receptor ligands: I. Involvement of dopamine autoreceptors. Life Sci. 1998;62(7):649-63.

REF 254

Indolebutylamines as selective 5-HT(1A) agonists. J Med Chem. 2004 Sep 9;47(19):4677-83.

REF 255

Drug Development in Schizophrenia: Summary and Table. Pharmaceutical Medicine October 2014, Volume 28, Issue 5, pp 265-271

REF 256

EFFICACY AND SAFETY OF NOVEL DOPAMINE SEROTONIN STABILIZER RP 5063 IN ACUTE SCHIZOPHRENIA AND SCHIZOAFFECTIVE DISORDER. Schizophrenia Research Volume 153, Supplement 1, April 2014, Pages S22.

REF 257

DOI: 10.1038/sj.mp.4002062

REF 258

Double-blind study of the actively transported levodopa prodrug XP21279 in Parkinson's disease. Mov Disord. 2014 Jan;29(1):75-82.

REF 259

7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602). J Med Chem. 1998 Dec 31;41(27):5402-9.

REF 260

Pharmacological characteristics of ATI-9242, a Novel Atypical Antipsychotic. FASEB J, April, 2010, 24(Meeting Abstract Supplement),773.12.

REF 261

Neurohumoral response to carmoxirole, a selective dopamine (D2) receptor agonist, in patients with chronic moderate heart failure. Cardiovasc Drugs Ther. 1998 Sep;12(4):387-94.

REF 262

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031195)

REF 263

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031909)

REF 264

Bi-directional modulation of BNST neurons by 5-HT: Molecular expression and functional properties of excitatory 5-HT receptor subtypes. Neuroscience. 2009 December 29; 164(4): 1776-1793.

REF 265

SSR181507, a dopamine D receptor and 5-HT() receptor ligand: evidence for mixed anxiolytic- and antidepressant-like activities.Pharmacol Biochem Behav.2011 Jan;97(3):428-35.

REF 266

The effects of umespirone as a potential anxiolytic and antipsychotic agent. Pharmacol Biochem Behav. 1991 Sep;40(1):89-96.

REF 267

Modeling of brain D2 receptor occupancy-plasma concentration relationships with a novel antipsychotic, YKP1358, using serial PET scans in healthy volunteers. Clin Pharmacol Ther. 2007 Feb;81(2):252-8.

REF 268

Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017).Expert Opin Ther Pat. 2018 Mar;28(3):175-196.

REF 269

Novel serotonin receptor 2 (5-HT2R) agonists and antagonists: a patent review (2004-2014).Expert Opin Ther Pat. 2016;26(1):89-106.

REF 270

Dopamine uptake inhibiting versus dopamine releasing properties of fencamfamine: an in vitro study. Biochem Pharmacol. 1983 Aug 1;32(15):2329-31.

REF 271

A role for medial prefrontal dopaminergic innervation in instrumental conditioning. J Neurosci. 2009 May 20;29(20):6599-606.

REF 272

Pharmacologically induced, subsecond dopamine transients in the caudate-putamen of the anesthetized rat. Synapse. 2007 Jan;61(1):37-9.

REF 273

Dopamine D2 receptors: a potential pharmacological target for nomifensine and tranylcypromine but not other antidepressant treatments. Pharmacol Biochem Behav. 1995 Aug;51(4):565-9.

REF 274

Remoxipride in Parkinson's disease: differential response in patients with dyskinesias fluctuations versus psychosis. Clin Neuropharmacol. 1995 Feb;18(1):39-45.

REF 275

Effect of sertindole on extracellular dopamine, acetylcholine, and glutamate in the medial prefrontal cortex of conscious rats: a comparison with r... Psychopharmacology (Berl). 2009 Sep;206(1):39-49.

REF 276

Dopamine D2(High) receptors moderately elevated by sertindole. Synapse. 2008 May;62(5):389-93.

REF 277

Bifeprunox: a partial agonist at dopamine D2 and serotonin 1A receptors, influences nicotine-seeking behaviour in response to drug-associated stimuli in rats.Addict Biol.2012 Mar;17(2):274-86.

REF 278

Emerging drugs for bipolar disorder. Expert Opin Emerg Drugs. 2006 Nov;11(4):621-34.

REF 279

Effect of nolomirole on monocrotaline-induced heart failure. Pharmacol Res. 2004 Jan;49(1):1-5.

REF 280

The role of the novel D2/beta2-agonist, Viozan (sibenadet HCl), in the treatment of symptoms of chronic obstructive pulmonary disease: results of a... Respir Med. 2003 Jan;97 Suppl A:S23-33.

REF 281

3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.

REF 282

Therapeutic effects of dopamine D1/D2 receptor agonists on detrusor hyperreflexia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned parkinso... J Pharmacol Exp Ther. 1998 Jul;286(1):228-33.

REF 283

Pharmacokinetics and central nervous system toxicity of declopramide (3-chloroprocainamide) in rats and mice. Anticancer Drugs. 1999 Jan;10(1):79-88.

REF 284

A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. J Med Chem. 1994 Apr 15;37(8):1060-2.

REF 285

Comparison between the pharmacology of dopamine receptors mediating the inhibition of cell firing in rat brain slices through the substantia nigra pars compacta and ventral tegmental area. Br J Pharmacol. 1994 Jul;112(3):873-80.

REF 286

CA patent application no. 648479, Implants for the treatment of dopamine associated states.

REF 287

Savoxepine: striatal dopamine-D2 receptor occupancy in human volunteers measured using positron emission tomography (PET). Eur J Clin Pharmacol. 1993;44(2):135-40.

REF 288

SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition. Bioorg Med Chem Lett. 2003 Feb 10;13(3):405-8.

REF 289

Clinical pipeline report, company report or official report of Avarx.

REF 290

A comparison of the neuro-endocrinological and temperature effects of DU 29894, flesinoxan, sulpiride and haloperidol in normal volunteers. Br J Clin Pharmacol. 1995 Jan;39(1):7-14.

REF 291

The dopaminergic stabilizers pridopidine and ordopidine enhance cortico-striatal Arc gene expression. J Neural Transm. 2014 Nov;121(11):1337-47.

REF 292

S18327 (1-[2-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)piperid-1-yl]ethyl]3-phenyl imidazolin-2-one), a novel, potential antipsychotic displaying marked antagonist properties at alpha(1)- and alpha(2)-adrenergic receptors: I. Receptorial, neurochemical, and electrophysiological profile. J Pharmacol Exp Ther. 2000 Jan;292(1):38-53.

REF 293

SDZ GLC 756, a novel octahydrobenzo[g]quinoline derivative exerts opposing effects on dopamine D1 and D2 receptors. J Neural Transm. 1996;103(1-2):17-30.

REF 294

Synthesis and dual D2 and 5-HT1A receptor binding affinities of 7-piperazinyl and 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones. Med Chem. 2014;10(5):484-96.

REF 295

F15063, a potential antipsychotic with dopamine D(2)/D(3) antagonist, 5-HT(1A) agonist and D(4) partial agonist properties: (IV) duration of brain D2-like receptor occupancy and antipsychotic-like activity versus plasma concentration in mice.Naunyn Schmiedebergs Arch Pharmacol.2007 Jun;375(4):241-50.

REF 296

Schizophrenia, "just the facts" 5. Treatment and prevention. Past, present, and future. Schizophr Res. 2010 Sep;122(1-3):1-23.

REF 297

(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist. J Med Chem. 1990 Nov;33(11):2948-50.

REF 298

Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.

REF 299

ACP-103, a 5-HT2A/2C inverse agonist, potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and nucleus accumbens. Psychopharmacology (Berl). 2005 Dec;183(2):144-53.

REF 300

BIMG 80, a novel potential antipsychotic drug: evidence for multireceptor actions and preferential release of dopamine in prefrontal cortex. J Neurochem. 1997 Jul;69(1):182-90.

REF 301

CGP 25454A, a novel and selective presynaptic dopamine autoreceptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):230-8.

REF 302

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025558)

REF 303

Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole. J Neurochem. 2003 Nov;87(3):631-41.

REF 304

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)

REF 305

WO patent application no. 2009,0568,11, Medicaments.

REF 306

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005079)

REF 307

Dopamine D4 receptors in human postmortem brain tissue of normal and schizophrenic subjects. An [3]NGD-94-1 study. Schizophrenia Research Volume 29, Issues 1-2, January 1998, Pages 93.

REF 308

Synthesis and pharmacological evaluation of the enantiomers of the dopamine autoreceptor agonist PD 135385, Bioorg. Med. Chem. Lett. 3(4):639-644 (1993).

REF 309

Piperazinylalkyl heterocycles as potential antipsychotic agents. J Med Chem. 1995 Oct 13;38(21):4198-210.

REF 310

Neuroleptic properties of Y-20024, a new benzofurancarboxamide derivative. Nihon Yakurigaku Zasshi. 1989 Nov;94(5):269-80.

REF 311

Displacement activity of bisbenzylisoquinoline alkaloids at striatal 3H-SCH 23390 and 3H-raclopride binding sites. J Nat Prod. 1992 Sep;55(9):1281-6.

REF 312

Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands. J Med Chem. 2005 Jan 13;48(1):266-73.

REF 313

Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin secretion and catalepsy. J Pharmacol Exp Ther. 1995 Nov;275(2):885-98.

REF 314

Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.

REF 315

Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. J Med Chem. 1993 Oct 15;36(21):3188-96.

REF 316

Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonis... J Med Chem. 2000 Feb 24;43(4):756-62.

REF 317

Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. J Med Chem. 2009 Jun 11;52(11):3548-62.

REF 318

3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure... J Med Chem. 1996 Oct 11;39(21):4285-98.

REF 319

Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine. J Nat Prod. 1998 Jun 26;61(6):709-12.

REF 320

R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30.

REF 321

Synthesis and dopamine receptor affinities of N-alkyl-11-hydroxy-2-methoxynoraporphines: N-alkyl substituents determine D1 versus D2 receptor selec... J Med Chem. 2008 Feb 28;51(4):983-7.

REF 322

Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines. Bioorg Med Chem. 2008 Apr 1;16(7):3773-9.

REF 323

Advances in development of dopaminergic aporphinoids. J Med Chem. 2007 Jan 25;50(2):171-81.

REF 324

Synthesis and dopamine receptor affinities of enantiomers of 2-substituted apomorphines and their N-n-propyl analogues. J Med Chem. 1990 Jun;33(6):1800-5.

REF 325

Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors. J Med Chem. 2010 Jun 24;53(12):4803-7.

REF 326

Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2955-9.

REF 327

Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand. Bioorg Med Chem. 2007 Sep 1;15(17):5811-8.

REF 328

Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition. J Med Chem. 2006 Nov 2;49(22):6607-13.

REF 329

Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands. J Med Chem. 1991 Oct;34(10):2946-53.

REF 330

Piperidinylpyrroles: design, synthesis and binding properties of novel and selective dopamine D4 receptor ligands. Bioorg Med Chem Lett. 1999 Nov 1;9(21):3143-6.

REF 331

Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1982 Jul;25(7):855-8.

REF 332

D4 dopamine receptor-selective compounds from the Chinese plant Phoebe chekiangensis, Bioorg. Med. Chem. Lett. 7(9):1207-1212 (1997).

REF 333

Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity, Bioorg. Med. Chem. Lett. 7(3):241-246 (1997).

REF 334

New N-n-propyl-substituted 3-aryl- and 3-cyclohexylpiperidines as partial agonists at the D4 dopamine receptor. J Med Chem. 2003 Jan 2;46(1):161-8.

REF 335

Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines. Bioorg Med Chem. 2008 Apr 15;16(8):4563-8.

REF 336

Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists. J Med Chem. 1981 Sep;24(9):1107-10.

REF 337

Halogenated boldine derivatives with enhanced monoamine receptor selectivity. J Nat Prod. 2000 Apr;63(4):480-4.

REF 338

N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and rece... J Med Chem. 1998 Dec 3;41(25):4933-8.

REF 339

New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template. Bioorg Med Chem Lett. 1999 Sep 6;9(17):2593-8.

REF 340

New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80.

REF 341

3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4... J Med Chem. 1996 May 10;39(10):1941-2.

REF 342

Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). ... J Med Chem. 1990 Mar;33(3):1015-22.

REF 343

6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. J Med Chem. 1992 Oct 30;35(22):3984-90.

REF 344

Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.

REF 345

Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a... J Med Chem. 2010 Feb 11;53(3):1023-37.

REF 346

Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives. Bioorg Med Chem Lett. 2006 Feb;16(3):490-4.

REF 347

Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.genes... Bioorg Med Chem Lett. 2006 Feb;16(3):658-62.

REF 348

Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.

REF 349

Evaluation of the effects of the enantiomers of reduced haloperidol, azaperol, and related 4-amino-1-arylbutanols on dopamine and sigma receptors. J Med Chem. 1993 Nov 26;36(24):3929-36.

REF 350

Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotoni... J Med Chem. 2003 Feb 27;46(5):702-15.

REF 351

18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography. J Med Chem. 1993 Nov 12;36(23):3707-20.

REF 352

Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly... J Med Chem. 2008 May 22;51(10):3005-19.

REF 353

Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding character... J Med Chem. 2008 Dec 25;51(24):7806-19.

REF 354

Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-... Bioorg Med Chem. 2009 Jun 1;17(11):3923-33.

REF 355

Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template... Bioorg Med Chem. 2010 Aug 1;18(15):5661-74.

REF 356

Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT. J Med Chem. 1993 Jan 22;36(2):221-8.

REF 357

Substituted 5-amino-4,5,6,7-tetrahydroindazoles as partial ergoline structures with dopaminergic activity. J Med Chem. 1989 Oct;32(10):2388-96.

REF 358

Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds. J Med Chem. 1990 Apr;33(4):1155-63.

REF 359

2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. J Med Chem. 1987 Nov;30(11):2099-104.

REF 360

Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. J Med Chem. 1989 Dec;32(12):2573-82.

REF 361

Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. J Med Chem. 1980 Jun;23(6):635-43.

REF 362

Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. J Med Chem. 1997 Dec 5;40(25):4146-53.

REF 363

Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6.

REF 364

Synthesis and characterization of selective dopamine D2 receptor antagonists. 2. Azaindole, benzofuran, and benzothiophene analogs of L-741,626. Bioorg Med Chem. 2010 Jul 15;18(14):5291-300.

REF 365

Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor act... J Med Chem. 2008 Sep 25;51(18):5813-22.

REF 366

Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines. Bioorg Med Chem Lett. 2009 Jan 1;19(1):51-3.

REF 367

Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010.

REF 368

Discovery and characterization of a G protein-biased agonist that inhibits beta-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol. 2014 Jul;86(1):96-105.

REF 369

N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists. Bioorg Med Chem. 2009 Jul 1;17(13):4756-62.

REF 370

A functional test identifies dopamine agonists selective for D3 versus D2 receptors. Neuroreport. 1995 Jan 26;6(2):329-32.

REF 371

Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for (1)-adre... J Med Chem. 2010 Oct 14;53(19):7021-34.

REF 372

Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907. J Pharmacol Exp Ther. 1995 Dec;275(3):1355-66.

REF 373

Isoindolinone enantiomers having affinity for the dopamine D4 receptor. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1499-502.

REF 374

Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3... J Med Chem. 2007 Aug 23;50(17):4135-46.

REF 375

Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804.

REF 376

Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine recepto... J Med Chem. 1995 Jan 20;38(2):318-27.

REF 377

Atropisomeric derivatives of 2',6'-disubstituted (R)-11-phenylaporphine: selective serotonin 5-HT(7) receptor antagonists. J Med Chem. 2001 Apr 26;44(9):1337-40.

REF 378

Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43.

REF 379

A new mechanism of allostery in a G protein-coupled receptor dimer. Nat Chem Biol. 2014 Sep;10(9):745-52.

REF 380

Synthesis and pharmacological characterization of 1-phenyl-, 4-phenyl-, and 1-benzyl-1,2,3,4-tetrahydroisoquinolines as dopamine receptor ligands. J Med Chem. 1988 Oct;31(10):1941-6.

REF 381

Effects of the partial dopamine receptor agonists SDZ 208-911, SDZ 208-912 and terguride on central monoamine receptors. A behavioral, biochemical and electrophysiological study. Naunyn SchmiedebergsArch Pharmacol. 1991 Sep;344(3):263-74.

REF 382

trans-10,11-dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine: a highly potent selective dopamine D1 full agonist. J Med Chem. 1990 Jun;33(6):1756-64.

REF 383

Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent benzot... J Med Chem. 1987 Jul;30(7):1166-76.

REF 384

Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential a... J Med Chem. 2005 Nov 3;48(22):6855-69.

REF 385

Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key frag... J Med Chem. 2007 Aug 9;50(16):3883-90.

REF 386

Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities Bioorg Med Chem. 2009 Oct 1;17(19):6898-907.

REF 387

(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists, Bioorg. Med. Chem. Lett. 7(21):2759-2764 (1997).

REF 388

N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. J Med Chem. 1997 Apr 11;40(8):1252-7.

REF 389

Effect of dopamine receptor agonists on sensory nerve activity: possible therapeutic targets for the treatment of asthma and COPD. Br J Pharmacol. 2002 Jun;136(4):620-8.

REF 390

Discovery of beta-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93.

REF 391

Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists. Bioorg Med Chem. 2009 Jul 15;17(14):5153-63.

REF 392

Nonconserved residues in the second transmembrane-spanning domain of the D(4) dopamine receptor are molecular determinants of D(4)-selective pharmacology. Mol Pharmacol. 2000 Jan;57(1):144-52.

REF 393

Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors. J Med Chem. 1992 Feb 7;35(3):423-30.

REF 394

Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues. Br J Pharmacol. 2000 Jul;130(5):1045-59.

REF 395

Structure of a D2 dopamine receptor-G-protein complex in a lipid membrane. Nature. 2020 Aug;584(7819):125-129.

REF 396

Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone. Nature. 2018 Mar 8;555(7695):269-273.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Yuzong CHEN

Prof. Feng ZHU