Target Validation Information
TTD ID T32060
Target Name 5-HT 2A receptor (HTR2A)
Type of Target
Successful
Drug Potency against Target Drug Info Ki = 73 nM [57]
Blonanserin Drug Info Ki = 5460 nM [64]
Flibanserin Drug Info Ki = 49 nM
Iloperidone Drug Info KI = 11 nM [62]
Lurasidone hydrochloride Drug Info Ki = 2.03 nM [60]
Ocaperidone Drug Info Ki = 0.14 nM [59]
Pimavanserin Drug Info Ki = 8 nM [61]
SR46349B Drug Info Ki = 1.26 nM [63]
1192U90 Drug Info Ki = 3.3 nM [65]
YM-992 Drug Info Ki = 21 nM [58]
Drug Info Ki = 160 nM [47]
Drug Info Ki = 429 nM [10]
Drug Info Ki = 69 nM [16]
Drug Info Ki = 1040 nM [5]
Drug Info Ki = 48 nM [40]
Drug Info Ki = 588 nM [10]
Drug Info Ki = 70 nM [48]
Drug Info Ki = 2100 nM [48]
Drug Info IC50 = 26 nM [50]
Drug Info Ki = 3500 nM [47]
Drug Info Ki = 44 nM [20]
Drug Info Ki = 0.88 nM [17]
Drug Info Ki = 1158 nM [32]
Drug Info Ki = 2512 nM
Drug Info Ki = 351 nM [30]
Drug Info Ki = 3870 nM [8]
Drug Info Ki = 2550 nM [7]
Drug Info Ki = 500 nM [7]
Drug Info Ki = 1164 nM [26]
Drug Info IC50 = 2.08 nM [14]
Drug Info Ki = 100 nM [30]
Drug Info Ki = 46 nM [29]
(+/-)-nantenine Drug Info Ki = 832 nM [39]
(1-Phenethyl-piperidin-4-yl)-phenyl-methanone Drug Info Ki = 9.6 nM [2]
(2-Indol-1-yl-ethyl)-dimethyl-amine Drug Info Ki = 650 nM [5]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info Ki = 0.78 nM [27]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 89 nM [27]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 82 nM [27]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info IC50 = 1.91 nM [14]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info Ki = 7.7 nM [22]
(E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridine Drug Info Ki = 7.4 nM [22]
(R)-(-)-11-hydroxy-N-n-propylnoraporphine Drug Info Ki = 114 nM [33]
(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine Drug Info IC50 = 0.46 nM [23]
(R)-3-(4-propylmorpholin-2-yl)phenol Drug Info Ki = 970 nM [25]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info Ki = 159 nM
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 200 nM
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 159 nM
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info Ki = 794 nM
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 251 nM
(S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info Ki = 1120 nM [16]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 100 nM
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info Ki = 11100 nM [48]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 635 nM [5]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info Ki = 98 nM [42]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info Ki = 28 nM [42]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info Ki = 45 nM [42]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info Ki = 20 nM [42]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info Ki = 31 nM [42]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info IC50 = 0.58 nM [14]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info IC50 = 0.54 nM [14]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info IC50 = 0.73 nM [14]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info IC50 = 1.68 nM [14]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info IC50 = 0.74 nM [14]
1-(10-Bromoanthracen-9-yl)-2-aminopropane Drug Info Ki = 313 nM [30]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info Ki = 4710 nM [47]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info Ki = 8430 nM [47]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info Ki = 5200 nM [30]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info IC50 = 0.77 nM [14]
1-(2-Methoxy-phenyl)-4-propyl-piperazine Drug Info Ki = 3290 nM [52]
1-(3-(phenylthio)propyl)-4-m-tolylpiperazine Drug Info Ki = 13.6 nM [19]
1-(4-Bromo-2,5-difluorophenyl)-2-aminopropane Drug Info Ki = 2505 nM [30]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info Ki = 2430 nM [47]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 310 nM [10]
1-Butyl-4-(2-methoxy-phenyl)-piperazine Drug Info Ki = 2280 nM [52]
1-Ethyl-4-(2-methoxy-phenyl)-piperazine Drug Info Ki = 3120 nM [52]
1-Methyl-1,3-dihydro-indol-2-one Drug Info Ki = 25 nM [4]
1-naphthylpiperazine Drug Info Ki = 18 nM [48]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info Ki = 569 nM
11-Butyryloxy-N-n-propylnoraporphine Drug Info Ki = 56 nM [33]
11-Heptanoyloxy-N-n-propylnoraporphine Drug Info Ki = 95 nM [33]
11-Hexanoyloxy-N-n-propylnoraporphine Drug Info Ki = 109 nM [33]
11-Propionyloxy-N-n-propylnoraporphine Drug Info Ki = 109 nM [33]
11-valeryloxynoraporphine Drug Info Ki = 92 nM [33]
2,2-Diphenyl-ethylamine Drug Info Ki = 5700 nM [3]
2-(1H-indol-3-yl)-N,N-dimethylethanamine Drug Info Ki = 1636 nM [30]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info Ki = 210 nM [49]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 8130 nM [49]
2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamine Drug Info Ki = 59 nM [30]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 7850 nM [49]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 4870 nM [49]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info Ki = 4650 nM [49]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine Drug Info Ki = 2095 nM
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info IC50 = 2 nM [14]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Drug Info Ki = 92 nM [36]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info Ki = 21 nM [38]
2-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 1367 nM [32]
2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indole Drug Info Ki = 2.7 nM [1]
2-Phenyl-3-piperidin-4-yl-1H-indole Drug Info Ki = 12.1 nM [1]
2-Piperazin-1-yl-phenol Drug Info Ki = 17200 nM [47]
3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 28 nM [1]
3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 7.8 nM [1]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 0.5 nM [1]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info IC50 = 3.5 nM [14]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info Ki = 900 nM [10]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info Ki = 7600 nM [10]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info Ki = 122 nM [10]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 982 nM [10]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info Ki = 8480 nM [47]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info Ki = 498 nM [10]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info Ki = 923 nM [10]
3-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 7.5 nM [32]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info Ki = 113 nM
3-Naphthalen-1-yl-pyrrolidine Drug Info Ki = 40 nM
4,4-Diphenylbutan-1-amine Drug Info Ki = 2589 nM [36]
4-(10H-Anthracen-9-ylidene)-1-methyl-piperidine Drug Info Ki = 0.7 nM [3]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [43]
4-(4-Fluoro-benzyl)-piperidine hydrochloride Drug Info Ki = 1100 nM [8]
4-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 124 nM [32]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 434 nM [26]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 80 nM [7]
5-MEO-DMT Drug Info IC50 = 9.53 nM [14]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 75 nM [7]
5-METHOXYTRYPTAMINE Drug Info Ki = 14 nM [46]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info Ki = 93 nM [29]
6-bromoaplysinopsin Drug Info Ki = 2000 nM [6]
6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 330 nM [5]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info Ki = 794 nM
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1400 nM [7]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info Ki = 99 nM [29]
7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 80 nM [5]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 2200 nM [7]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 21 nM [7]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 115 nM [7]
8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 320 nM [5]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 400 nM [7]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info Ki = 1200 nM [48]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info Ki = 310 nM [48]
9-(2-aminoethyl)-9,10-dihydroanthracene Drug Info Ki = 480 nM [36]
9-(2-aminopropyl)-9,10-dihydroanthracene Drug Info Ki = 32 nM [36]
9-(Aminomethyl)-9,10-dihydroanthracene Drug Info Ki = 20 nM [3]
9-(N-benzylaminomethyl)-9,10-dihydroanthracene Drug Info Ki = 721 nM [41]
A-80426 Drug Info Ki = 144 nM [12]
ALTANSERIN Drug Info Ki = 0.72 nM [34]
Aplysinopsin Drug Info Ki = 598 nM
BARETTIN Drug Info Ki = 1930 nM [18]
Brolamfetamine Drug Info Ki = 13 nM [31]
C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamine Drug Info Ki = 47 nM [17]
C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamine Drug Info Ki = 4125 nM [3]
C-(9H-Thioxanthen-9-yl)-methylamine Drug Info Ki = 65 nM [3]
C-(9H-Xanthen-9-yl)-methylamine Drug Info Ki = 170 nM [3]
CINANSERIN Drug Info Ki = 4 nM [46]
DOM Drug Info Ki = 100 nM [30]
FLUANISONE Drug Info Ki = 52 nM [45]
GR-127935 Drug Info Ki = 42.7 nM [11]
ISOCLOZAPINE Drug Info IC50 = 12 nM [56]
LYSERGIC ACID DIETHYLAMIDE Drug Info Ki = 3.5 nM [16]
M100907 Drug Info Ki = 0.36 nM [34]
MAZAPERTINE Drug Info Ki = 165 nM [51]
MDL-11939 Drug Info Ki = 12.5 nM [8]
MDL-28161 Drug Info IC50 = 0.9 nM [8]
MESCALINE Drug Info Ki = 5500 nM [30]
N,N-dimethyl-2,2-diphenylethanamine Drug Info Ki = 7356 nM [36]
N,N-Dimethyl-3,3-diphenylpropan-1-amine Drug Info Ki = 1636 nM [36]
N,N-dimethyl-4,4-diphenylbutan-1-amine Drug Info Ki = 1151 nM [36]
N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamide Drug Info Ki = 248 nM [21]
N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 110 nM [21]
N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamide Drug Info Ki = 462 nM [20]
N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 53 nM [20]
N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 223 nM [20]
N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 278 nM [20]
N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamide Drug Info Ki = 487 nM [21]
N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 213 nM [21]
N-(1-phenethylpiperidin-4-yl)-1-naphthamide Drug Info Ki = 543 nM [21]
N-(1-phenethylpiperidin-4-yl)-2-naphthamide Drug Info Ki = 42 nM [21]
N-3'-ethylaplysinopsin Drug Info Ki = 1700 nM [6]
N-methyl-3,3-diphenylpropan-1-amine Drug Info Ki = 1498 nM [36]
N-methyl-4,4-diphenylbutan-1-amine Drug Info Ki = 754 nM [36]
NELOTANSERIN Drug Info Ki = 0.51 nM [44]
PG-01037 Drug Info Ki = 62.4 nM [24]
PHENETHYLAMINE Drug Info Ki = 16820 nM [3]
PRUVANSERIN Drug Info Ki = 0.48 nM [44]
PRUVANSERIN Drug Info Ki = 0.87 nM [15]
PSILOCIN Drug Info Ki = 323 nM [30]
QUIPAZINE Drug Info Ki = 794 nM [37]
Racemic DOI Drug Info Ki = 19 nM [30]
Racemic DOTFM Drug Info Ki = 33 nM [30]
Ro-60-0175 Drug Info Ki = 39 nM [27]
RP-68303 Drug Info IC50 = 30 nM [53]
SB-271046 Drug Info Ki = 1740 nM [28]
SEROTONIN Drug Info Ki = 1258 nM [37]
TIOSPIRONE Drug Info Ki = 0.58 nM [54]
TRYPTAMINE Drug Info Ki = 50 nM [46]
TRYPTOLINE Drug Info Ki = 3000 nM [7]
VER-2692 Drug Info Ki = 31 nM [13]
VER-3323 Drug Info Ki = 351 nM [9]
VER-5384 Drug Info Ki = 112 nM [9]
VER-5593 Drug Info Ki = 53 nM [9]
WAY-208466 Drug Info IC50 = 351 nM [35]
YM-348 Drug Info Ki = 13 nM [29]
ZOTEPINE Drug Info Ki = 2.7 nM [2]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 335 nM [10]
[3H]spiperone Drug Info Ki = 1 nM [55]
References
REF 1 3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists. Bioorg Med Chem Lett. 2000 Dec 18;10(24):2701-3.
REF 2 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
REF 3 Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin rec... Bioorg Med Chem Lett. 2001 Feb 26;11(4):563-6.
REF 4 Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity. Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31.
REF 5 Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors. Bioorg Med Chem Lett. 2002 Jan 21;12(2):155-8.
REF 6 New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea. J Nat Prod. 2002 Apr;65(4):476-80.
REF 7 Binding of beta-carbolines at 5-HT(2) serotonin receptors. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4421-5.
REF 8 Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding. J Med Chem. 1992 Dec 25;35(26):4903-10.
REF 9 Indoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.
REF 10 SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.
REF 11 Synthesis of potent and selective serotonin 5-HT1B receptor ligands. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.
REF 12 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 13 Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2006 Feb;16(3):677-80.
REF 14 1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. J Med Chem. 2006 Jan 12;49(1):318-28.
REF 15 A new class of selective, non-basic 5-HT2A receptor antagonists. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3201-4.
REF 16 C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor. J Med Chem. 2006 Jul 13;49(14):4269-74.
REF 17 1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agoni... J Med Chem. 2006 Sep 21;49(19):5794-803.
REF 18 Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4.
REF 19 Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1708-12.
REF 20 Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the a... Bioorg Med Chem Lett. 2007 Mar 15;17(6):1570-4.
REF 21 Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the ... Bioorg Med Chem Lett. 2007 Mar 15;17(6):1565-9.
REF 22 2,5-Disubstituted pyridines: the discovery of a novel series of 5-HT2A ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2643-8.
REF 23 Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2998-3002.
REF 24 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 25 Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6691-6.
REF 26 Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61.
REF 27 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 a... Bioorg Med Chem. 2008 Feb 15;16(4):1966-82.
REF 28 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 29 Synthesis and structure-activity relationships of a series of benzazepine derivatives as 5-HT2C receptor agonists. Bioorg Med Chem. 2008 Mar 15;16(6):3309-20.
REF 30 The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands. Bioorg Med Chem. 2008 Apr 15;16(8):4661-9.
REF 31 'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines. Bioorg Med Chem. 2008 Jun 1;16(11):6242-51.
REF 32 Methoxy-substituted 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives exhibit differential binding affinities at the 5-HT(2A) receptor. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5268-71.
REF 33 N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands. Bioorg Med Chem. 2008 Sep 15;16(18):8335-8.
REF 34 Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET. Bioorg Med Chem. 2009 Apr 15;17(8):2989-3002.
REF 35 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 36 Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity. Bioorg Med Chem. 2009 Sep 15;17(18):6496-504.
REF 37 Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.
REF 38 Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. Bioorg Med Chem Lett. 2010 Jan 1;20(1):266-71.
REF 39 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 40 Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33.
REF 41 9-Aminomethyl-9,10-dihydroanthracene (AMDA) analogs as structural probes for steric tolerance in 5-HT2A and H1 receptor binding sites. Bioorg Med Chem Lett. 2010 Feb 1;20(3):935-8.
REF 42 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 43 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 44 Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. J Med Chem. 2010 Aug 12;53(15):5696-706.
REF 45 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. J Med Chem. 1987 Nov;30(11):2099-104.
REF 46 Central serotonin receptors as targets for drug research. J Med Chem. 1987 Jan;30(1):1-12.
REF 47 Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents. J Med Chem. 1986 May;29(5):630-4.
REF 48 5-HT1 and 5-HT2 binding characteristics of some quipazine analogues. J Med Chem. 1986 Nov;29(11):2375-80.
REF 49 5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues. J Med Chem. 1986 Feb;29(2):194-9.
REF 50 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-... J Med Chem. 1985 Oct;28(10):1540-2.
REF 51 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 52 Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new ... J Med Chem. 1994 Aug 19;37(17):2754-60.
REF 53 New indole derivatives as potent and selective serotonin uptake inhibitors. J Med Chem. 1993 Apr 30;36(9):1194-202.
REF 54 3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. J Med Chem. 1996 Jan 5;39(1):143-8.
REF 55 Activity of Parthenolide at 5HT2A receptors. J Nat Prod. 1997 Jun;60(6):651-3.
REF 56 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 57 Synthesis 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 58 Serotonin 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 59 In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Mol Pharmacol. 1992 Mar;41(3):494-508.
REF 60 Lurasidone (SM-13496), a novel atypical antipsychotic drug, reverses MK-801-induced impairment of learning and memory in the rat passive-avoidance ... Eur J Pharmacol. 2007 Oct 31;572(2-3):160-70.
REF 61 5-HT(2A) inverse-agonists for the treatment of insomnia. Curr Top Med Chem. 2008;8(11):969-76.
REF 62 The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. J Pharmacol Exp Ther. 1995 Sep;274(3):1404-13.
REF 63 (1-(2,5-dimethoxy-4 iodophenyl)-2-aminopropane)-induced head-twitches in the rat are mediated by 5-hydroxytryptamine (5-HT) 2A receptors: modulation by novel 5-HT2A/2C antagonists, D1 antagonists and 5-HT1A agonists. J Pharmacol Exp Ther. 1995 Apr;273(1):101-12.
REF 64 Pharmacological profile of AD-5423, a novel antipsychotic with both potent dopamine-D2 and serotonin-S2 antagonist properties. J Pharmacol Exp Ther. 1993 Jan;264(1):158-65.
REF 65 Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents. J Med Chem. 1996 Nov 22;39(24):4692-703.

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