Target Information

Target General Infomation
Target ID
T32060
Former ID
TTDS00103
Target Name
5-hydroxytryptamine 2A receptor
Gene Name
HTR2A
Synonyms
5-HT-2; 5-HT-2A; 5-HT2A receptor; 5-hydroxytryptamine receptor 2A; Serotonin receptor; Serotonin receptor 2A; HTR2A
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Addiction [ICD code not available]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Central nervous system disease [ICD10: G00-G99]
Cardiovascular disorder [ICD10: I00-I99]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Depression [ICD9: 311; ICD10: F30-F39]
Erythropoietic porphyria [ICD10: E80.0]
Fibromyalgia [ICD9: 729.1; ICD10: M79.7]
Female sexual dysfunction [ICD9: 302.7; ICD10: F52]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Hypertension [ICD9: 401; ICD10: I10-I16]
Hemorrhoids [ICD10: I84]
Migraine [ICD9: 346; ICD10: G43]
Mood disorder [ICD10: F30-F39]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99]
Pancreatitis [ICD9: 577.0-577.1; ICD10: K85, K86.0K86.1]
Parkinson's disease; Psychosis; Schizophrenia [ICD9:290-299, 332, 295; ICD10: F02.3, F20-F29, G20, F20]
Parkinson disease psychosis [ICD10: G00-G99]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Schizophrenia [ICD9: 295; ICD10: F20]
Sleep disorders [ICD9: 307.4, 327, 780.5; ICD10: F51, G47]
Schizophrenia; Sleep maintenance insomnia [ICD9:295, 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F20, F51.0, G47.0]
Schizophrenia; Schizoaffective disorders [ICD9: 295, 295.70; ICD10: F20, F25]
Sleep initiation and maintenance disorders; Primary insomnia; Schizophrenia [ICD9: 295, 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F20, F51.0, G47.0]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
Unspecified [ICD code not available]
Function
G-protein coupled receptor for5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5- dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.
BioChemical Class
GPCR rhodopsin
Target Validation
T32060
UniProt ID
P28223
Sequence
MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK
SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
Drugs and Mode of Action
Drug(s) Abilify Maintena Drug Info Approved Erythropoietic porphyria [551871]
Aniracetam Drug Info Approved Cerebrovascular ischaemia [467478], [526084]
Flibanserin Drug Info Approved Mood disorder [532651], [542987]
Iloperidone Drug Info Approved Schizophrenia [530677], [543255]
Lurasidone hydrochloride Drug Info Approved Schizophrenia [530859], [531351], [542486], [551871]
Pimavanserin Drug Info Approved Parkinson disease psychosis [889440]
Sarpogrelate Drug Info Approved Diabetes [535855], [539330]
ZOTEPINE Drug Info Approved Anxiety disorder [538628], [551871]
Blonanserin Drug Info Phase 3 Schizophrenia [536463], [542649]
Flibanserin Drug Info Phase 3 Female sexual dysfunction [536493], [542987]
ITI-007 Drug Info Phase 3 Schizophrenia; Sleep maintenance insomnia [525226], [549912]
Low dose ITI-007 Drug Info Phase 3 Schizophrenia [548546]
M100907 Drug Info Phase 3 Sleep disorders [522054]
Pimavanserin Drug Info Phase 3 Parkinson's disease; Psychosis; Schizophrenia [543125], [547301]
SR46349B Drug Info Phase 3 Sleep initiation and maintenance disorders; Primary insomnia; Schizophrenia [536463]
TNX-102 Drug Info Phase 3 Fibromyalgia [547624]
TRYPTAMINE Drug Info Phase 3 Discovery agent [521730], [538764]
VOLINANSERIN Drug Info Phase 3 Discovery agent [522480], [539159]
Zicronapine Drug Info Phase 3 Schizophrenia [523357]
BVT.28949 Drug Info Phase 2 Glaucoma [548204]
Ocaperidone Drug Info Phase 2 Schizophrenia; Schizoaffective disorders [467839], [526792], [536463]
PRUVANSERIN Drug Info Phase 2 Sleep disorders [521764]
1192U90 Drug Info Phase 1 Psychotic disorders [534252]
Abaperidone Drug Info Phase 1 Schizophrenia [551815]
MIN-101 Drug Info Phase 1 Schizophrenia [524902]
SKL-10406 Drug Info Phase 1 Major depressive disorder [549136]
Temanogrel Drug Info Phase 1 Cardiovascular disorder [524599]
YKP-1358 Drug Info Phase 1 Schizophrenia; Schizoaffective disorders [536463]
Org-23366 Drug Info Preclinical Schizophrenia [536463]
LYSERGIC ACID DIETHYLAMIDE Drug Info Withdrawn from market Addiction [526769], [539053]
Deramciclane Drug Info Discontinued in Phase 3 Anxiety disorder [540889], [544913]
Iferanserin-Ventrus Drug Info Discontinued in Phase 3 Hemorrhoids [547235]
MDL-11939 Drug Info Discontinued in Phase 3 Anxiety disorder [539169], [544618]
Ritanserin Drug Info Discontinued in Phase 3 Anxiety disorder [543335], [544590]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [538617], [544679]
Adatanserin Drug Info Discontinued in Phase 2 Severe mood disorders [536580]
AMESERGIDE Drug Info Discontinued in Phase 2 Mood disorder [539285], [544787]
ATI-9242 Drug Info Discontinued in Phase 2 Schizophrenia [548733]
FCE-22716 Drug Info Discontinued in Phase 2 Hypertension [533340]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [545274]
NELOTANSERIN Drug Info Discontinued in Phase 2 Sleep disorders [548083]
SERAZAPINE HYDROCHLORIDE Drug Info Discontinued in Phase 2 Anxiety disorder [544867]
SERGOLEXOLE MALEATE Drug Info Discontinued in Phase 2 Migraine [544716]
SL65.0472 Drug Info Discontinued in Phase 2 Cardiovascular disorder [547242]
YM-992 Drug Info Discontinued in Phase 2 Depression [546447]
AM-831 Drug Info Discontinued in Phase 1 Schizophrenia [547459]
DUP-734 Drug Info Discontinued in Phase 1 Psychotic disorders [544981]
1192U90 Drug Info Terminated Schizophrenia [536463]
A-80426 Drug Info Terminated Discovery agent [546043]
AMPEROZIDE Drug Info Terminated Alcohol use disorders [544701]
DV-7028 Drug Info Terminated Cardiovascular disorder [545055]
Fananserin Drug Info Terminated Schizophrenia [536463], [540837]
GMC-283 Drug Info Terminated Schizophrenia [536463]
ICI-169369 Drug Info Terminated Anxiety disorder [539780], [544709]
LY53857 Drug Info Terminated Discovery agent [539138], [544876]
MDL-28161 Drug Info Terminated Discovery agent [544961]
R-102444 Drug Info Terminated Pancreatitis [547365]
Ro-60-0175 Drug Info Terminated Discovery agent [539026], [546467]
RP-68303 Drug Info Terminated Discovery agent [545423]
ZD-3638 Drug Info Terminated Schizophrenia [536463]
Agonist (+)-LSD Drug Info [527178]
3,4-Methylenedioxymethamphetamine Drug Info [551382]
5-CT Drug Info [527178]
Abilify Maintena Drug Info [526792], [527134]
ACP-106 Drug Info [526792]
AL-37350A Drug Info [526713]
alpha-methyl-5-HT Drug Info [525890]
AM-831 Drug Info [550322]
BRL-15572 Drug Info [534475]
BW723C86 Drug Info [527178]
DV-7028 Drug Info [537955], [538116], [538117]
LP-12 Drug Info [528956]
LP-44 Drug Info [528956]
m-chlorophenylpiperazine Drug Info [534830]
MMDA Drug Info [551393]
N-1-isopropyl-5-MeOT Drug Info [533905]
N-1-isopropyltryptamine Drug Info [533905]
Org 12962 Drug Info [527178]
SB 216641 Drug Info [534475]
Temanogrel Drug Info [526792], [550267]
TFMPP Drug Info [527178]
[125I]DOI Drug Info [525927]
Inhibitor (+/-)-nantenine Drug Info [530558]
(1-Phenethyl-piperidin-4-yl)-phenyl-methanone Drug Info [525963]
(2-Indol-1-yl-ethyl)-dimethyl-amine Drug Info [526235]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info [529168]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [529168]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [529168]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info [527952]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info [528690]
(E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridine Drug Info [528690]
(R)-(+)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info [528294]
(R)-(-)-11-hydroxy-N-n-propylnoraporphine Drug Info [529686]
(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine Drug Info [528778]
(R)-3-(4-propylmorpholin-2-yl)phenol Drug Info [529128]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info [528294]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info [533482]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info [526235]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info [530927]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info [530927]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info [527952]
1-(10-Bromoanthracen-9-yl)-2-aminopropane Drug Info [529336]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info [533476]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info [533476]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info [529336]
1-(2,6-dimethoxy-4-methylphenyl)propan-2-amine Drug Info [529336]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info [527952]
1-(2-Methoxy-phenyl)-4-propyl-piperazine Drug Info [533873]
1-(2-Methoxy-phenyl)-piperazine Drug Info [533476]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [529013]
1-(3-(phenylthio)propyl)-4-m-tolylpiperazine Drug Info [528625]
1-(3-Trifluoromethyl-phenyl)-piperazine Drug Info [533476]
1-(4-Bromo-2,5-difluorophenyl)-2-aminopropane Drug Info [529336]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info [533476]
1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amine Drug Info [529336]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info [527668]
1-Butyl-4-(2-methoxy-phenyl)-piperazine Drug Info [533873]
1-Ethyl-4-(2-methoxy-phenyl)-piperazine Drug Info [533873]
1-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [529672]
1-Methyl-1,3-dihydro-indol-2-one Drug Info [526055]
1-Naphthalen-1-yl-piperazine Drug Info [533482]
1-Naphthalen-2-yl-piperazine Drug Info [533482]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info [551334]
11-Butyryloxy-N-n-propylnoraporphine Drug Info [529686]
11-Heptanoyloxy-N-n-propylnoraporphine Drug Info [529686]
11-Hexanoyloxy-N-n-propylnoraporphine Drug Info [529686]
11-Propionyloxy-N-n-propylnoraporphine Drug Info [529686]
11-valeryloxynoraporphine Drug Info [529686]
2,2-Diphenyl-ethylamine Drug Info [525993]
2,5-dimethoxy-4-bromophenethylamine Drug Info [528433]
2-(1H-indol-3-yl)-N,N-dimethylethanamine Drug Info [529336]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info [533498]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamine Drug Info [529336]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info [533498]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine Drug Info [551319]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info [527952]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Drug Info [530331]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info [530516]
2-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [529672]
2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indole Drug Info [525940]
2-Phenyl-3-piperidin-4-yl-1H-indole Drug Info [525940]
2-Piperazin-1-yl-phenol Drug Info [533476]
3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [525940]
3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [525940]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [525940]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info [527952]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info [527668]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info [527668]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info [527668]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [527668]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info [527668]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [527668]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info [533476]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info [527668]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info [527668]
3-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [529672]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info [551334]
3-Naphthalen-1-yl-pyrrolidine Drug Info [551334]
4,4-Diphenylbutan-1-amine Drug Info [530331]
4-(10H-Anthracen-9-ylidene)-1-methyl-piperidine Drug Info [525993]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-(4-Fluoro-benzyl)-piperidine hydrochloride Drug Info [526959]
4-Benzyl-1-methyl-piperidine hydrochloride Drug Info [526959]
4-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [529672]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526899]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [551219]
5-MEO-DMT Drug Info [527952]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526899]
5-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info [526899]
5-METHOXYTRYPTAMINE Drug Info [533464]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info [529221]
6-bromoaplysinopsin Drug Info [526321]
6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info [526235]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [551219]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526899]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info [529221]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info [529221]
7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info [526235]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526899]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526899]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info [526899]
8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info [526235]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526899]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info [533482]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info [533482]
8-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info [526899]
9-(2-aminoethyl)-9,10-dihydroanthracene Drug Info [530331]
9-(2-aminopropyl)-9,10-dihydroanthracene Drug Info [530331]
9-(Aminomethyl)-9,10-dihydroanthracene Drug Info [525993]
9-(N-benzylaminomethyl)-9,10-dihydroanthracene Drug Info [530613]
A-80426 Drug Info [527799]
A-987306 Drug Info [529789]
ALTANSERIN Drug Info [530045]
Aniracetam Drug Info [551390]
APLYSINOPSIN Drug Info [551219]
BARETTIN Drug Info [528498]
Brolamfetamine Drug Info [529463]
C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamine Drug Info [528433]
C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamine Drug Info [525993]
C-(9H-Thioxanthen-9-yl)-methylamine Drug Info [525993]
C-(9H-Xanthen-9-yl)-methylamine Drug Info [525993]
CHLOROPHENYLPIPERAZINE Drug Info [530589]
CINANSERIN Drug Info [533464]
Dimethyltryptamine Drug Info [551401]
DOM Drug Info [529336]
Etisulergine Drug Info [533501]
FLUANISONE Drug Info [533378]
ISOCLOZAPINE Drug Info [534532]
LY433222 Drug Info [536286]
LYSERGIC ACID DIETHYLAMIDE Drug Info [528294]
MAZAPERTINE Drug Info [533800]
MDL-11939 Drug Info [526959]
MDL-28161 Drug Info [526959]
MESCALINE Drug Info [529336]
N,N-dimethyl-2,2-diphenylethanamine Drug Info [530331]
N,N-Dimethyl-3,3-diphenylpropan-1-amine Drug Info [530331]
N,N-dimethyl-4,4-diphenylbutan-1-amine Drug Info [530331]
N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamide Drug Info [528639]
N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamide Drug Info [528639]
N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamide Drug Info [528638]
N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info [528638]
N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info [528638]
N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamide Drug Info [528638]
N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamide Drug Info [528639]
N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamide Drug Info [528639]
N-(1-benzylpiperidine-4-yl)-2-naphthamide Drug Info [528638]
N-(1-phenethylpiperidin-4-yl)-1-naphthamide Drug Info [528639]
N-(1-phenethylpiperidin-4-yl)-2-naphthamide Drug Info [528639]
N-3'-ethylaplysinopsin Drug Info [526321]
N-methyl-3,3-diphenylpropan-1-amine Drug Info [530331]
N-methyl-4,4-diphenylbutan-1-amine Drug Info [530331]
PG-01037 Drug Info [528974]
PHENETHYLAMINE Drug Info [525993]
PHENYLPIPERAZINE Drug Info [533482]
PSILOCIN Drug Info [529336]
QUIPAZINE Drug Info [530451]
Racemic DOI Drug Info [529336]
Racemic DOTFM Drug Info [529336]
Ro-60-0175 Drug Info [529168]
RP-68303 Drug Info [534052]
SB-271046 Drug Info [529191]
SEROTONIN Drug Info [530451]
SPIPERONE Drug Info [534417]
TIOSPIRONE Drug Info [534093]
TRYPTAMINE Drug Info [533464]
TRYPTOLINE Drug Info [526899]
VER-2692 Drug Info [527833]
VER-3323 Drug Info [527037]
VER-5384 Drug Info [527037]
VER-5593 Drug Info [527037]
VOLINANSERIN Drug Info [530045]
WAY-208466 Drug Info [530209]
YM-348 Drug Info [529221]
YM-992 Drug Info [536286]
ZOTEPINE Drug Info [525963]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [527668]
[2-(6-Methoxy-indol-1-yl)-ethyl]-dimethyl-amine Drug Info [526235]
Antagonist 1192U90 Drug Info [536463]
9-OH-risperidone Drug Info [534281]
Adatanserin Drug Info [534942], [536580]
AMESERGIDE Drug Info [526792], [533907]
Blonanserin Drug Info [536463]
bufotenine Drug Info [534136]
BVT.28949 Drug Info [526792], [544175]
cyamemazine Drug Info [526510]
EGIS-7625 Drug Info [527053]
Fananserin Drug Info [536463]
FCE-22716 Drug Info [526792], [533340]
GMC-283 Drug Info [536463]
Iloperidone Drug Info [530677], [536463]
ITI-007 Drug Info [551041]
Low dose ITI-007 Drug Info [526792], [551041]
LY063518 Drug Info [534232]
LY108742 Drug Info [533905]
LY215840 Drug Info [533905]
LY314228 Drug Info [534232]
LY320954 Drug Info [534232]
LY53857 Drug Info [535896], [535927], [536352], [538142]
LY86057 Drug Info [533905]
M100907 Drug Info [535134]
metergoline Drug Info [527178]
MIN-101 Drug Info [526792]
MPDT Drug Info [525722]
norfluoxetine Drug Info [525929]
Org-23366 Drug Info [536463]
Ritanserin Drug Info [536752], [536787], [538142]
Sarpogrelate Drug Info [537172], [537535], [538037]
SB 215505 Drug Info [525458]
SB 221284 Drug Info [527178]
SB 228357 Drug Info [525730]
SB 242084 Drug Info [534428]
SERAZAPINE HYDROCHLORIDE Drug Info [526792], [533896]
SERGOLEXOLE MALEATE Drug Info [526792], [533252]
spiramide Drug Info [527178]
TNX-102 Drug Info [551739]
[11C]volinanserin Drug Info [525893]
[18F]altanserin Drug Info [534323]
[3H]fananserin Drug Info [534046]
[3H]N-methylspiperone Drug Info [525890]
Modulator Abaperidone Drug Info [553290]
AMPEROZIDE Drug Info
ATI-9242 Drug Info [526792], [550651]
Deramciclane Drug Info [534609]
DUP-734 Drug Info
EPLIVANSERIN MESILATE Drug Info
Flibanserin Drug Info [532651]
ICI-169369 Drug Info
Iferanserin-Ventrus Drug Info [543891]
Lurasidone hydrochloride Drug Info [530859], [531351]
NELOTANSERIN Drug Info
Ocaperidone Drug Info [526792]
Pimavanserin Drug Info
PRUVANSERIN Drug Info [552847]
R-102444 Drug Info [535964]
SEL-73 Drug Info [526792]
SL65.0472 Drug Info
SR46349B Drug Info
Very low dose (VLD) cyclobenzaprine Drug Info [526792]
YKP-1358 Drug Info [528644]
Zicronapine Drug Info [549861]
Binder SKL-10406 Drug Info [544111]
ZD-3638 Drug Info [536463]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Gap junction
Serotonergic synapse
Inflammatory mediator regulation of TRP channels
PANTHER Pathway 5HT2 type receptor mediated signaling pathway
Reactome Serotonin receptors
G alpha (q) signalling events
WikiPathways Serotonin Receptor 2 and STAT3 Signaling
Serotonin Receptor 2 and ELK-SRF/GATA4 signaling
SIDS Susceptibility Pathways
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 467478(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: 4133).
Ref 467839(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: 46).
Ref 521730ClinicalTrials.gov (NCT00227136) Effect of Oral 5-HTP Intake on Urinary 5-HIAA Excretion. U.S. National Institutes of Health.
Ref 521764ClinicalTrials.gov (NCT00259311) Efficacy Study of LY2422347 to Treat Insomnia. U.S. National Institutes of Health.
Ref 522054ClinicalTrials.gov (NCT00495885) Efficacy and Safety of M100907 on Sleep Maintenance Insomnia With a Sub-study in Stable Type II Diabetes Mellitus. U.S. National Institutes of Health.
Ref 522480ClinicalTrials.gov (NCT00788515) Comparison of Volinanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties. U.S. National Institutes of Health.
Ref 523357ClinicalTrials.gov (NCT01295372) Safety and Efficacy of Zicronapine in Patients With Schizophrenia. U.S. National Institutes of Health.
Ref 524599ClinicalTrials.gov (NCT02034292) Safety Study of APD-791 With Aspirin and/or Clopidogrel. U.S. National Institutes of Health.
Ref 524902ClinicalTrials.gov (NCT02232529) Pharmacokinetic Study of MIN-101 in Healthy Subjects. U.S. National Institutes of Health.
Ref 525226ClinicalTrials.gov (NCT02469155) A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment.
Ref 526084Anxiolytic 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 526769Psychopathology and psychophysiology of minimal LSD-25 dosage; a preliminary dosage-response spectrum. AMA Arch Neurol Psychiatry. 1958 Feb;79(2):208-10.
Ref 526792Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 530859Pharmacological 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 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 533340Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
Ref 5342521192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42.
Ref 535855A 50-year history of new drugs in Japan-the development and trends of hemostatics and antithrombotic drugs. Yakushigaku Zasshi. 2003;38(1):93-105.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536493Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 538617(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: 101).
Ref 538628(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: 103).
Ref 538764(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: 125).
Ref 539026(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: 166).
Ref 539053(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: 17).
Ref 539138(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: 183).
Ref 539159(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: 185).
Ref 539169(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: 186).
Ref 539285(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: 199).
Ref 539330(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: 210).
Ref 539780(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: 273).
Ref 540837(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: 5434).
Ref 540889(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: 5490).
Ref 542486(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: 7461).
Ref 542649(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: 7670).
Ref 542987(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: 8182).
Ref 543125(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: 8423).
Ref 543255(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: 87).
Ref 543335(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: 97).
Ref 544590Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000237)
Ref 544618Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000314)
Ref 544679Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000562)
Ref 544701Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000669)
Ref 544709Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000690)
Ref 544716Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000706)
Ref 544787Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001117)
Ref 544867Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001373)
Ref 544876Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001395)
Ref 544913Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001479)
Ref 544961Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001723)
Ref 544981Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001777)
Ref 545055Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001984)
Ref 545274Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662)
Ref 545423Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003204)
Ref 546043Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006017)
Ref 546447Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008166)
Ref 546467Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008324)
Ref 547235Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014343)
Ref 547242Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014358)
Ref 547301Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014997)
Ref 547365Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015510)
Ref 547459Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016551)
Ref 547624Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017946)
Ref 548083Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021795)
Ref 548204Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023041)
Ref 548546Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026498)
Ref 548733Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028165)
Ref 549136Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032727)
Ref 549912Clinical pipeline report, company report or official report of Intra-Cellular Therapies.
Ref 551815Small Molecule Therapeutics for Schizophrenia, Sylvain Celanire. Page(30).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 8894402016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76. doi: 10.1038/nrd.2017.14.
Ref 525458Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.
Ref 5257222-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
Ref 525730Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem. 2000 Mar 23;43(6):1123-34.
Ref 525890Differential modes of agonist binding to 5-hydroxytryptamine(2A) serotonin receptors revealed by mutation and molecular modeling of conserved residues in transmembrane region 5. Mol Pharmacol. 2000 Nov;58(5):877-86.
Ref 525893Autoradiographic localization of 5-HT(2A) receptors in the human brain using [(3)H]M100907 and [(11)C]M100907. Synapse. 2000 Dec 15;38(4):421-31.
Ref 525927Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem. 2000 Nov 30;43(24):4701-10.
Ref 525929Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications. Circulation. 2000 Dec 5;102(23):2836-41.
Ref 525940Bioorg Med Chem Lett. 2000 Dec 18;10(24):2701-3.3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
Ref 525963J Med Chem. 2001 Feb 15;44(4):477-501.Current and novel approaches to the drug treatment of schizophrenia.
Ref 525993Bioorg Med Chem Lett. 2001 Feb 26;11(4):563-6.Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.
Ref 526055Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31.Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity.
Ref 526235Bioorg Med Chem Lett. 2002 Jan 21;12(2):155-8.Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.
Ref 526321J Nat Prod. 2002 Apr;65(4):476-80.New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea.
Ref 526510Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
Ref 526713J Med Chem. 2003 Sep 11;46(19):4188-95.A novel and selective 5-HT2 receptor agonist with ocular hypotensive activity: (S)-(+)-1-(2-aminopropyl)-8,9-dihydropyrano[3,2-e]indole.
Ref 526792Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59.
Ref 526899Bioorg Med Chem Lett. 2003 Dec 15;13(24):4421-5.Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Ref 526959J Med Chem. 1992 Dec 25;35(26):4903-10.Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.
Ref 527037Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
Ref 527053Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34.
Ref 527134Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36.
Ref 527178Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. Epub 2004 Jul 30.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527799J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
Ref 527833Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Ref 528294J Med Chem. 2006 Jul 13;49(14):4269-74.C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.
Ref 528433J Med Chem. 2006 Sep 21;49(19):5794-803.1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.
Ref 528498J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Ref 528625Bioorg Med Chem Lett. 2007 Mar 15;17(6):1708-12. Epub 2006 Dec 23.Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines.
Ref 528638Bioorg Med Chem Lett. 2007 Mar 15;17(6):1570-4. Epub 2007 Jan 8.Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.
Ref 528639Bioorg Med Chem Lett. 2007 Mar 15;17(6):1565-9. Epub 2007 Jan 8.Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on the affinity for D2L, D4.2, and 5-HT2A receptors.
Ref 528644Modeling 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 528690Bioorg Med Chem Lett. 2007 May 1;17(9):2643-8. Epub 2007 Feb 2.2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands.
Ref 528778Bioorg Med Chem Lett. 2007 Jun 1;17(11):2998-3002. Epub 2007 Mar 25.Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity.
Ref 528956Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21. Epub 2007 Jul 25.
Ref 528974J Med Chem. 2007 Aug 23;50(17):4135-46. Epub 2007 Aug 2.Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
Ref 529013Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine.
Ref 529128Bioorg Med Chem Lett. 2007 Dec 15;17(24):6691-6. Epub 2007 Oct 22.Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.
Ref 529148Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation.
Ref 529168Bioorg Med Chem. 2008 Feb 15;16(4):1966-82. Epub 2007 Nov 4.Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
Ref 529191Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
Ref 529221Bioorg Med Chem. 2008 Mar 15;16(6):3309-20. Epub 2007 Dec 8.Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists.
Ref 529336Bioorg Med Chem. 2008 Apr 15;16(8):4661-9. Epub 2008 Feb 14.The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
Ref 529463Bioorg Med Chem. 2008 Jun 1;16(11):6242-51. Epub 2008 May 6.'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines.
Ref 529672Bioorg Med Chem Lett. 2008 Oct 1;18(19):5268-71. Epub 2008 Aug 22.Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor.
Ref 529686Bioorg Med Chem. 2008 Sep 15;16(18):8335-8. Epub 2008 Aug 28.N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Ref 530045Bioorg Med Chem. 2009 Apr 15;17(8):2989-3002. Epub 2009 Mar 14.Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Ref 530209Bioorg Med Chem. 2009 Jul 15;17(14):5153-63. Epub 2009 May 29.Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
Ref 530331Bioorg Med Chem. 2009 Sep 15;17(18):6496-504. Epub 2009 Aug 13.Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.
Ref 530451J Med Chem. 2009 Nov 12;52(21):6946-50.Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
Ref 530516Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71. Epub 2009 Oct 30.Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 530589Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. Epub 2009 Dec 6.Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.
Ref 530613Bioorg Med Chem Lett. 2010 Feb 1;20(3):935-8. Epub 2009 Dec 23.9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 530859Pharmacological 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 530927J Med Chem. 2010 Jun 24;53(12):4803-7.Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.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 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 5332525-Hydroxytryptamine2 receptor antagonist activity of the acid metabolite (1-isopropyl dihydrolysergic acid) of the ergoline ester, sergolexole (LY281067). J Pharmacol Exp Ther. 1989 Dec;251(3):1006-11.
Ref 533340Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
Ref 533378J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
Ref 533464J Med Chem. 1987 Jan;30(1):1-12.Central serotonin receptors as targets for drug research.
Ref 533476J Med Chem. 1986 May;29(5):630-4.Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.
Ref 533482J Med Chem. 1986 Nov;29(11):2375-80.5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
Ref 533498J Med Chem. 1986 Feb;29(2):194-9.5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues.
Ref 533501J Med Chem. 1985 Oct;28(10):1540-2.Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3 alpha, 4a alpha, 10a beta)-1,2,3,4,4a,5,10,10a- -octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamide.
Ref 533800J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Ref 533873J Med Chem. 1994 Aug 19;37(17):2754-60.Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new putative 5-HT1A receptor antagonist, and its analogs.
Ref 533896Serotonergic (5-HT2) mediation of anxiety-therapeutic effects of serazepine in generalized anxiety disorder. Biol Psychiatry. 1993 Jul 1-15;34(1-2):41-4.
Ref 533905Species variations in transmembrane region V of the 5-hydroxytryptamine type 2A receptor alter the structure-activity relationship of certain ergolines and tryptamines. Mol Pharmacol. 1994 Feb;45(2):277-86.
Ref 533907Effects of the serotonin antagonist amesergide on reproduction in female rats. Reprod Toxicol. 1993 Nov-Dec;7(6):607-12.
Ref 534046Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. Pharmacological characterization of [3H]RP 62203 binding in the rat brain. Eur J Pharmacol. 1993 Mar 16;233(1):37-45.
Ref 534052J Med Chem. 1993 Apr 30;36(9):1194-202.New indole derivatives as potent and selective serotonin uptake inhibitors.
Ref 534093J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Ref 534136Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. J Biol Chem. 1996 Jun 21;271(25):14672-5.
Ref 534232A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci. 1996;59(15):1259-68.
Ref 534281Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
Ref 534323Visualisation of loss of 5-HT2A receptors with age in healthy volunteers using [18F]altanserin and positron emission tomographic imaging. Psychiatry Res. 1996 Nov 25;68(1):11-22.
Ref 534417J Nat Prod. 1997 Jun;60(6):651-3.Activity of Parthenolide at 5HT2A receptors.
Ref 534428SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
Ref 534475SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
Ref 534532J Med Chem. 1997 Dec 5;40(25):4146-53.Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.
Ref 534609Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation. Psychopharmacology (Berl). 1998 Mar;136(2):99-104.
Ref 534830Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, -HT(2B) and 5-HT2C receptors. Naunyn Schmiedebergs Arch Pharmacol. 1999 Jan;359(1):1-6.
Ref 534942Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents. J Med Chem. 1999Dec 16;42(25):5077-94.
Ref 535134Antagonism of 5-hydroxytryptamine(2a) receptors attenuates the behavioral effects of cocaine in rats. J Pharmacol Exp Ther. 2001 Apr;297(1):357-63.
Ref 535896The fenfluramine metabolite (+)-norfenfluramine is vasoactive. J Pharmacol Exp Ther. 2004 May;309(2):845-52. Epub 2004 Jan 29.
Ref 535927Some studies on the 5-hydroxytryptamine receptors in the isolated rat uterus. Afr J Med Med Sci. 2002 Dec;31(4):361-5.
Ref 535964Effects of R-102444, an orally active 5-HT2A receptor antagonist, in rat models of peripheral vascular disease. Vascul Pharmacol. 2004 Feb;41(1):7-13.
Ref 536286Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23.
Ref 536352The 5-hydroxytryptamine2A receptor is involved in (+)-norfenfluramine-induced arterial contraction and blood pressure increase in deoxycorticosterone acetate-salt hypertension. J Pharmacol Exp Ther. 2007 May;321(2):485-91. Epub 2007 Feb 8.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 536752Human embryonic stem cell-derived oligodendrocyte progenitor cells express the serotonin receptor and are susceptible to JC virus infection. J Virol. 2008 Sep;82(17):8896-9. Epub 2008 Jun 25.
Ref 536787Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7. Epub 2008 Jul 4.
Ref 537172Acute effects of sarpogrelate, a 5-HT2A receptor antagonist on cytokine production in endotoxin shock model of rats. Eur J Pharmacol. 2009 Jul 1;614(1-3):122-7. Epub 2009 Mar 24.
Ref 537535Beneficial effects of sarpogrelate hydrochloride, a 5-HT2A receptor antagonist, supplemented with pioglitazone on diabetic model mice. Endocr Res. 2009;34(1-2):18-30.
Ref 537955Evidence that 5-HT2A receptors are not involved in 5-HT-mediated thermoregulation in mice. Pharmacol Biochem Behav. 1995 Dec;52(4):755-8.
Ref 538037Therapeutic effect of sarpogrelate, a new 5-hydroxytryptamine receptor 2A antagonist, on diabetic nephropathy and neuropathy. Nephron. 1997;76(2):227-9.
Ref 538116A potent 5-hydroxytryptamine receptor (5-HT2A) antagonist, DV-7028, delays arterial thrombosis development in rats. Thromb Res. 1998 Jun 15;90(6):259-70.
Ref 538117Vascular and cardiac effects of DV-7028, a selective, 5-HT2-receptor antagonist in rats. J Cardiovasc Pharmacol. 1998 Aug;32(2):266-73.
Ref 538142p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.
Ref 543891(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. (Target id: 6).
Ref 544111Bi-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 544175Novel ocular antihypertensive compounds in clinical trials. Clin Ophthalmol. 2011; 5: 667-677.
Ref 549861Clinical pipeline report, company report or official report of Lundbeck.
Ref 550267Clinical pipeline report, company report or official report of Arena Pharmaceuticals.
Ref 550322Clinical pipeline report, company report or official report of Avarx.
Ref 550651Pharmacological characteristics of ATI-9242, a Novel Atypical Antipsychotic. FASEB J, April, 2010, 24(Meeting Abstract Supplement),773.12.
Ref 551041Clinical pipeline report, company report or official report of Intra-Cellular Therapies, Inc.
Ref 551219Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes. Bioorg Med Chem. 2010 Jul 1;18(13):4783-92. doi: 10.1016/j.bmc.2010.05.017. Epub 2010 May 15.
Ref 5513194-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists, Bioorg. Med. Chem. Lett. 7(13):1635-1638 (1997).
Ref 551334Regioselective 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 551382The origin of <span class="caps">MDMA</span> (ecstasy) revisited: the true story reconstructed from the original documents. Addiction. 2006 Sep;101(9):1241-5.
Ref 551390Anxiolytic 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 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551401Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects. Arch Gen Psychiatry. 1994 Feb;51(2):85-97.
Ref 551739Clinical pipeline report, company report or official report of Tonix Pharmaceuticals.
Ref 5528475-HT(2A) inverse-agonists for the treatment of insomnia. Curr Top Med Chem. 2008;8(11):969-76.
Ref 5532907-[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.

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