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 Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Addiction [ICD code not available]
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]
Female sexual dysfunction [ICD9: 302.7; ICD10: F52]
Fibromyalgia [ICD9: 729.1; ICD10: M79.7]
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]
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]
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
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]
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 [1]
Aniracetam Drug Info Approved Cerebrovascular ischaemia [2], [3]
Flibanserin Drug Info Approved Mood disorder [4], [5]
Iloperidone Drug Info Approved Schizophrenia [6], [7]
Lurasidone hydrochloride Drug Info Approved Schizophrenia [8], [9], [10], [1]
Pimavanserin Drug Info Approved Parkinson disease psychosis [11]
Sarpogrelate Drug Info Approved Diabetes [12], [13]
ZOTEPINE Drug Info Approved Anxiety disorder [14], [1]
Blonanserin Drug Info Phase 3 Schizophrenia [15], [16]
Flibanserin Drug Info Phase 3 Female sexual dysfunction [17], [5]
ITI-007 Drug Info Phase 3 Schizophrenia; Sleep maintenance insomnia [18], [19]
Low dose ITI-007 Drug Info Phase 3 Schizophrenia [20]
M100907 Drug Info Phase 3 Sleep disorders [21]
Pimavanserin Drug Info Phase 3 Parkinson's disease; Psychosis; Schizophrenia [22], [23]
SR46349B Drug Info Phase 3 Sleep initiation and maintenance disorders; Primary insomnia; Schizophrenia [15]
TNX-102 Drug Info Phase 3 Fibromyalgia [24]
TRYPTAMINE Drug Info Phase 3 Discovery agent [25], [26]
VOLINANSERIN Drug Info Phase 3 Discovery agent [27], [28]
Zicronapine Drug Info Phase 3 Schizophrenia [29]
BVT.28949 Drug Info Phase 2 Glaucoma [30]
Ocaperidone Drug Info Phase 2 Schizophrenia; Schizoaffective disorders [31], [32], [15]
PRUVANSERIN Drug Info Phase 2 Sleep disorders [33]
1192U90 Drug Info Phase 1 Psychotic disorders [34]
Abaperidone Drug Info Phase 1 Schizophrenia [35]
MIN-101 Drug Info Phase 1 Schizophrenia [36]
SKL-10406 Drug Info Phase 1 Major depressive disorder [37]
Temanogrel Drug Info Phase 1 Cardiovascular disorder [38]
YKP-1358 Drug Info Phase 1 Schizophrenia; Schizoaffective disorders [15]
Org-23366 Drug Info Preclinical Schizophrenia [15]
LYSERGIC ACID DIETHYLAMIDE Drug Info Withdrawn from market Addiction [39], [40]
Deramciclane Drug Info Discontinued in Phase 3 Anxiety disorder [41], [42]
Iferanserin-Ventrus Drug Info Discontinued in Phase 3 Hemorrhoids [43]
MDL-11939 Drug Info Discontinued in Phase 3 Anxiety disorder [44], [45]
Ritanserin Drug Info Discontinued in Phase 3 Anxiety disorder [46], [47]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [48], [49]
Adatanserin Drug Info Discontinued in Phase 2 Severe mood disorders [50]
AMESERGIDE Drug Info Discontinued in Phase 2 Mood disorder [51], [52]
ATI-9242 Drug Info Discontinued in Phase 2 Schizophrenia [53]
FCE-22716 Drug Info Discontinued in Phase 2 Hypertension [54]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [55]
NELOTANSERIN Drug Info Discontinued in Phase 2 Sleep disorders [56]
SERAZAPINE HYDROCHLORIDE Drug Info Discontinued in Phase 2 Anxiety disorder [57]
SERGOLEXOLE MALEATE Drug Info Discontinued in Phase 2 Migraine [58]
SL65.0472 Drug Info Discontinued in Phase 2 Cardiovascular disorder [59]
YM-992 Drug Info Discontinued in Phase 2 Depression [60]
AM-831 Drug Info Discontinued in Phase 1 Schizophrenia [61]
DUP-734 Drug Info Discontinued in Phase 1 Psychotic disorders [62]
1192U90 Drug Info Terminated Schizophrenia [15]
A-80426 Drug Info Terminated Discovery agent [63]
AMPEROZIDE Drug Info Terminated Alcohol use disorders [64]
DV-7028 Drug Info Terminated Cardiovascular disorder [65]
Fananserin Drug Info Terminated Schizophrenia [15], [66]
GMC-283 Drug Info Terminated Schizophrenia [15]
ICI-169369 Drug Info Terminated Anxiety disorder [67], [68]
LY53857 Drug Info Terminated Discovery agent [69], [70]
MDL-28161 Drug Info Terminated Discovery agent [71]
R-102444 Drug Info Terminated Pancreatitis [72]
Ro-60-0175 Drug Info Terminated Discovery agent [73], [74]
RP-68303 Drug Info Terminated Discovery agent [75]
ZD-3638 Drug Info Terminated Schizophrenia [15]
Agonist (+)-LSD Drug Info [76]
3,4-Methylenedioxymethamphetamine Drug Info [77]
5-CT Drug Info [76]
Abilify Maintena Drug Info [32], [78]
ACP-106 Drug Info [32]
AL-37350A Drug Info [79]
alpha-methyl-5-HT Drug Info [80]
AM-831 Drug Info [81]
BRL-15572 Drug Info [82]
BW723C86 Drug Info [76]
DV-7028 Drug Info [83], [84], [85]
LP-12 Drug Info [86]
LP-44 Drug Info [86]
m-chlorophenylpiperazine Drug Info [87]
MMDA Drug Info [88]
N-1-isopropyl-5-MeOT Drug Info [89]
N-1-isopropyltryptamine Drug Info [89]
Org 12962 Drug Info [76]
SB 216641 Drug Info [82]
Temanogrel Drug Info [32], [90]
TFMPP Drug Info [76]
[125I]DOI Drug Info [91]
Inhibitor (+/-)-nantenine Drug Info [92]
(1-Phenethyl-piperidin-4-yl)-phenyl-methanone Drug Info [93]
(2-Indol-1-yl-ethyl)-dimethyl-amine Drug Info [94]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info [95]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [95]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [95]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info [96]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info [97]
(E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridine Drug Info [97]
(R)-(+)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info [98]
(R)-(-)-11-hydroxy-N-n-propylnoraporphine Drug Info [99]
(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine Drug Info [100]
(R)-3-(4-propylmorpholin-2-yl)phenol Drug Info [101]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info [102]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info [102]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [102]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info [102]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [102]
(S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info [98]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info [102]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info [103]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info [94]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info [104]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info [104]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info [104]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info [104]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info [104]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info [96]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [96]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info [96]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info [96]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info [96]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info [96]
1-(10-Bromoanthracen-9-yl)-2-aminopropane Drug Info [105]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info [106]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info [106]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info [105]
1-(2,6-dimethoxy-4-methylphenyl)propan-2-amine Drug Info [105]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info [96]
1-(2-Methoxy-phenyl)-4-propyl-piperazine Drug Info [107]
1-(2-Methoxy-phenyl)-piperazine Drug Info [106]
1-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [108]
1-(3-(phenylthio)propyl)-4-m-tolylpiperazine Drug Info [109]
1-(3-Trifluoromethyl-phenyl)-piperazine Drug Info [106]
1-(4-Bromo-2,5-difluorophenyl)-2-aminopropane Drug Info [105]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info [106]
1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amine Drug Info [105]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info [110]
1-Butyl-4-(2-methoxy-phenyl)-piperazine Drug Info [107]
1-Ethyl-4-(2-methoxy-phenyl)-piperazine Drug Info [107]
1-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [111]
1-Methyl-1,3-dihydro-indol-2-one Drug Info [112]
1-Naphthalen-1-yl-piperazine Drug Info [103]
1-Naphthalen-2-yl-piperazine Drug Info [103]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info [113]
11-Butyryloxy-N-n-propylnoraporphine Drug Info [99]
11-Heptanoyloxy-N-n-propylnoraporphine Drug Info [99]
11-Hexanoyloxy-N-n-propylnoraporphine Drug Info [99]
11-Propionyloxy-N-n-propylnoraporphine Drug Info [99]
11-valeryloxynoraporphine Drug Info [99]
2,2-Diphenyl-ethylamine Drug Info [114]
2,5-dimethoxy-4-bromophenethylamine Drug Info [115]
2-(1H-indol-3-yl)-N,N-dimethylethanamine Drug Info [105]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info [116]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [116]
2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamine Drug Info [105]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info [116]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info [116]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info [116]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine Drug Info [117]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info [96]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Drug Info [118]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info [119]
2-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [111]
2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indole Drug Info [120]
2-Phenyl-3-piperidin-4-yl-1H-indole Drug Info [120]
2-Piperazin-1-yl-phenol Drug Info [106]
3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [120]
3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [120]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info [120]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info [96]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info [110]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info [110]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info [110]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [110]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info [110]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [110]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info [106]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info [110]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info [110]
3-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [111]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info [113]
3-Naphthalen-1-yl-pyrrolidine Drug Info [113]
4,4-Diphenylbutan-1-amine Drug Info [118]
4-(10H-Anthracen-9-ylidene)-1-methyl-piperidine Drug Info [114]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [121]
4-(4-Fluoro-benzyl)-piperidine hydrochloride Drug Info [122]
4-Benzyl-1-methyl-piperidine hydrochloride Drug Info [122]
4-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info [111]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [123]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [124]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [123]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [102]
5-MEO-DMT Drug Info [96]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [124]
5-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info [124]
5-METHOXYTRYPTAMINE Drug Info [125]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info [126]
6-bromoaplysinopsin Drug Info [127]
6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info [94]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [102]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [124]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info [126]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info [126]
7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info [94]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [124]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [124]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info [124]
8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info [94]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [124]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info [103]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info [103]
8-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info [124]
9-(2-aminoethyl)-9,10-dihydroanthracene Drug Info [118]
9-(2-aminopropyl)-9,10-dihydroanthracene Drug Info [118]
9-(Aminomethyl)-9,10-dihydroanthracene Drug Info [114]
9-(N-benzylaminomethyl)-9,10-dihydroanthracene Drug Info [128]
A-80426 Drug Info [129]
A-987306 Drug Info [130]
ALTANSERIN Drug Info [131]
Aniracetam Drug Info [132]
APLYSINOPSIN Drug Info [102]
BARETTIN Drug Info [133]
Brolamfetamine Drug Info [134]
C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamine Drug Info [115]
C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamine Drug Info [114]
C-(9H-Thioxanthen-9-yl)-methylamine Drug Info [114]
C-(9H-Xanthen-9-yl)-methylamine Drug Info [114]
CHLOROPHENYLPIPERAZINE Drug Info [135]
CINANSERIN Drug Info [125]
Dimethyltryptamine Drug Info [136]
DOM Drug Info [105]
Etisulergine Drug Info [137]
FLUANISONE Drug Info [138]
ISOCLOZAPINE Drug Info [139]
LY433222 Drug Info [140]
LYSERGIC ACID DIETHYLAMIDE Drug Info [98]
MAZAPERTINE Drug Info [141]
MDL-11939 Drug Info [122]
MDL-28161 Drug Info [122]
MESCALINE Drug Info [105]
N,N-dimethyl-2,2-diphenylethanamine Drug Info [118]
N,N-Dimethyl-3,3-diphenylpropan-1-amine Drug Info [118]
N,N-dimethyl-4,4-diphenylbutan-1-amine Drug Info [118]
N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamide Drug Info [142]
N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamide Drug Info [142]
N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamide Drug Info [143]
N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info [143]
N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info [143]
N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamide Drug Info [143]
N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamide Drug Info [142]
N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamide Drug Info [142]
N-(1-benzylpiperidine-4-yl)-2-naphthamide Drug Info [143]
N-(1-phenethylpiperidin-4-yl)-1-naphthamide Drug Info [142]
N-(1-phenethylpiperidin-4-yl)-2-naphthamide Drug Info [142]
N-3'-ethylaplysinopsin Drug Info [127]
N-methyl-3,3-diphenylpropan-1-amine Drug Info [118]
N-methyl-4,4-diphenylbutan-1-amine Drug Info [118]
PG-01037 Drug Info [144]
PHENETHYLAMINE Drug Info [114]
PHENYLPIPERAZINE Drug Info [103]
PSILOCIN Drug Info [105]
QUIPAZINE Drug Info [145]
Racemic DOI Drug Info [105]
Racemic DOTFM Drug Info [105]
Ro-60-0175 Drug Info [95]
RP-68303 Drug Info [146]
SB-271046 Drug Info [147]
SEROTONIN Drug Info [145]
SPIPERONE Drug Info [148]
TIOSPIRONE Drug Info [149]
TRYPTAMINE Drug Info [125]
TRYPTOLINE Drug Info [124]
VER-2692 Drug Info [150]
VER-3323 Drug Info [151]
VER-5384 Drug Info [151]
VER-5593 Drug Info [151]
VOLINANSERIN Drug Info [131]
WAY-208466 Drug Info [152]
YM-348 Drug Info [126]
YM-992 Drug Info [140]
ZOTEPINE Drug Info [93]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [110]
[2-(6-Methoxy-indol-1-yl)-ethyl]-dimethyl-amine Drug Info [94]
Antagonist 1192U90 Drug Info [15]
9-OH-risperidone Drug Info [153]
Adatanserin Drug Info [154], [50]
AMESERGIDE Drug Info [32], [155]
Blonanserin Drug Info [15]
bufotenine Drug Info [156]
BVT.28949 Drug Info [32], [157]
cyamemazine Drug Info [158]
EGIS-7625 Drug Info [159]
Fananserin Drug Info [15]
FCE-22716 Drug Info [32], [54]
GMC-283 Drug Info [15]
Iloperidone Drug Info [6], [15]
ITI-007 Drug Info [160]
Low dose ITI-007 Drug Info [32], [160]
LY063518 Drug Info [161]
LY108742 Drug Info [89]
LY215840 Drug Info [89]
LY314228 Drug Info [161]
LY320954 Drug Info [161]
LY53857 Drug Info [162], [163], [164], [165]
LY86057 Drug Info [89]
M100907 Drug Info [166]
metergoline Drug Info [76]
MIN-101 Drug Info [32]
MPDT Drug Info [167]
norfluoxetine Drug Info [168]
Org-23366 Drug Info [15]
Ritanserin Drug Info [169], [170], [165]
Sarpogrelate Drug Info [171], [172], [173]
SB 215505 Drug Info [174]
SB 221284 Drug Info [76]
SB 228357 Drug Info [175]
SB 242084 Drug Info [176]
SERAZAPINE HYDROCHLORIDE Drug Info [32], [177]
SERGOLEXOLE MALEATE Drug Info [32], [178]
spiramide Drug Info [76]
TNX-102 Drug Info [179]
[11C]volinanserin Drug Info [180]
[18F]altanserin Drug Info [181]
[3H]fananserin Drug Info [182]
[3H]N-methylspiperone Drug Info [80]
Modulator Abaperidone Drug Info [183]
AMPEROZIDE Drug Info
ATI-9242 Drug Info [32], [184]
Deramciclane Drug Info [185]
DUP-734 Drug Info
EPLIVANSERIN MESILATE Drug Info
Flibanserin Drug Info [4]
ICI-169369 Drug Info
Iferanserin-Ventrus Drug Info [186]
Lurasidone hydrochloride Drug Info [8], [9]
NELOTANSERIN Drug Info
Ocaperidone Drug Info [32]
Pimavanserin Drug Info
PRUVANSERIN Drug Info [187]
R-102444 Drug Info [188]
SEL-73 Drug Info [32]
SL65.0472 Drug Info
SR46349B Drug Info
Very low dose (VLD) cyclobenzaprine Drug Info [32]
YKP-1358 Drug Info [189]
Zicronapine Drug Info [190]
Binder SKL-10406 Drug Info [191]
ZD-3638 Drug Info [15]
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 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2(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 3Anxiolytic 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 42013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
REF 5(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 6Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
REF 7(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 8Pharmacological 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 9Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
REF 10(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 112016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76. doi: 10.1038/nrd.2017.14.
REF 12A 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 13(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 14(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 15The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
REF 16(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 17Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27.
REF 18ClinicalTrials.gov (NCT02469155) A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment.
REF 19Clinical pipeline report, company report or official report of Intra-Cellular Therapies.
REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026498)
REF 21ClinicalTrials.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 22(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 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014997)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017946)
REF 25ClinicalTrials.gov (NCT00227136) Effect of Oral 5-HTP Intake on Urinary 5-HIAA Excretion. U.S. National Institutes of Health.
REF 26(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 27ClinicalTrials.gov (NCT00788515) Comparison of Volinanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties. U.S. National Institutes of Health.
REF 28(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 29ClinicalTrials.gov (NCT01295372) Safety and Efficacy of Zicronapine in Patients With Schizophrenia. U.S. National Institutes of Health.
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023041)
REF 31(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 32Pharmacological profile of the new potent neuroleptic ocaperidone (R 79,598). J Pharmacol Exp Ther. 1992 Jan;260(1):146-59.
REF 33ClinicalTrials.gov (NCT00259311) Efficacy Study of LY2422347 to Treat Insomnia. U.S. National Institutes of Health.
REF 341192U90 in animal tests that predict antipsychotic efficacy, anxiolysis, and extrapyramidal side effects. Neuropsychopharmacology. 1996 Sep;15(3):231-42.
REF 35Small Molecule Therapeutics for Schizophrenia, Sylvain Celanire. Page(30).
REF 36ClinicalTrials.gov (NCT02232529) Pharmacokinetic Study of MIN-101 in Healthy Subjects. U.S. National Institutes of Health.
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032727)
REF 38ClinicalTrials.gov (NCT02034292) Safety Study of APD-791 With Aspirin and/or Clopidogrel. U.S. National Institutes of Health.
REF 39Psychopathology and psychophysiology of minimal LSD-25 dosage; a preliminary dosage-response spectrum. AMA Arch Neurol Psychiatry. 1958 Feb;79(2):208-10.
REF 40(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 41(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 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001479)
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014343)
REF 44(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 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000314)
REF 46(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 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000237)
REF 48(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 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000562)
REF 50Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
REF 51(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 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001117)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028165)
REF 54Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
REF 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662)
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021795)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001373)
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000706)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014358)
REF 60Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008166)
REF 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016551)
REF 62Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001777)
REF 63Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006017)
REF 64Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000669)
REF 65Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001984)
REF 66(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 67(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 68Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000690)
REF 69(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 70Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001395)
REF 71Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001723)
REF 72Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015510)
REF 73(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 74Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008324)
REF 75Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003204)
REF 76Pharmacological 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 77The 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 78Aripiprazole: a review of its use in schizophrenia and schizoaffective disorder. Drugs. 2004;64(15):1715-36.
REF 79J 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 80Differential 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 81Clinical pipeline report, company report or official report of Avarx.
REF 82SB-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 83Evidence that 5-HT2A receptors are not involved in 5-HT-mediated thermoregulation in mice. Pharmacol Biochem Behav. 1995 Dec;52(4):755-8.
REF 84A 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 85Vascular and cardiac effects of DV-7028, a selective, 5-HT2-receptor antagonist in rats. J Cardiovasc Pharmacol. 1998 Aug;32(2):266-73.
REF 86Structure-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 87Comparisons 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 88How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 89Species 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 90Clinical pipeline report, company report or official report of Arena Pharmaceuticals.
REF 91Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. J Med Chem. 2000 Nov 30;43(24):4701-10.
REF 92Bioorg 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 93J Med Chem. 2001 Feb 15;44(4):477-501.Current and novel approaches to the drug treatment of schizophrenia.
REF 94Bioorg Med Chem Lett. 2002 Jan 21;12(2):155-8.Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors.
REF 95Bioorg 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 96J 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 97Bioorg 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 98J 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 99Bioorg 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 100Bioorg 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 101Bioorg 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 102Synthesis 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 103J Med Chem. 1986 Nov;29(11):2375-80.5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
REF 104J 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 105Bioorg 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 106J Med Chem. 1986 May;29(5):630-4.Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.
REF 107J 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 108Bioorg 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 109Bioorg 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 110Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
REF 111Bioorg 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 112Bioorg 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 113Regioselective 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 114Bioorg 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 115J Med Chem. 2006 Sep 21;49(19):5794-803.1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.
REF 116J 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 1174-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists, Bioorg. Med. Chem. Lett. 7(13):1635-1638 (1997).
REF 118Bioorg 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 119Bioorg 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 120Bioorg 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 121J 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 122J Med Chem. 1992 Dec 25;35(26):4903-10.Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.
REF 123Bioorg 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 124Bioorg Med Chem Lett. 2003 Dec 15;13(24):4421-5.Binding of beta-carbolines at 5-HT(2) serotonin receptors.
REF 125J Med Chem. 1987 Jan;30(1):1-12.Central serotonin receptors as targets for drug research.
REF 126Bioorg 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 127J 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 128Bioorg 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 129J Med Chem. 2005 Oct 20;48(21):6523-43.Designed multiple ligands. An emerging drug discovery paradigm.
REF 130J 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 131Bioorg 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 132Anxiolytic 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 133J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
REF 134Bioorg Med Chem. 2008 Jun 1;16(11):6242-51. Epub 2008 May 6.'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines.
REF 135Bioorg 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 136Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects. Arch Gen Psychiatry. 1994 Feb;51(2):85-97.
REF 137J 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 138J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
REF 139J 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 140Serotonin 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 141J 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 142Bioorg 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 143Bioorg 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 144J 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 145J 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 146J Med Chem. 1993 Apr 30;36(9):1194-202.New indole derivatives as potent and selective serotonin uptake inhibitors.
REF 147Bioorg 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 148J Nat Prod. 1997 Jun;60(6):651-3.Activity of Parthenolide at 5HT2A receptors.
REF 149J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
REF 150Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
REF 151Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
REF 152Bioorg 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 153Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
REF 154Synthesis 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 155Effects of the serotonin antagonist amesergide on reproduction in female rats. Reprod Toxicol. 1993 Nov-Dec;7(6):607-12.
REF 156Mapping 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 157Novel ocular antihypertensive compounds in clinical trials. Clin Ophthalmol. 2011; 5: 667-677.
REF 158Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
REF 159Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34.
REF 160Clinical pipeline report, company report or official report of Intra-Cellular Therapies, Inc.
REF 161A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci. 1996;59(15):1259-68.
REF 162The fenfluramine metabolite (+)-norfenfluramine is vasoactive. J Pharmacol Exp Ther. 2004 May;309(2):845-52. Epub 2004 Jan 29.
REF 163Some studies on the 5-hydroxytryptamine receptors in the isolated rat uterus. Afr J Med Med Sci. 2002 Dec;31(4):361-5.
REF 164The 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 165p-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 166Antagonism of 5-hydroxytryptamine(2a) receptors attenuates the behavioral effects of cocaine in rats. J Pharmacol Exp Ther. 2001 Apr;297(1):357-63.
REF 1672-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
REF 168Evidence 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 169Human 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 170Characterization 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 171Acute 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 172Beneficial 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 173Therapeutic effect of sarpogrelate, a new 5-hydroxytryptamine receptor 2A antagonist, on diabetic nephropathy and neuropathy. Nephron. 1997;76(2):227-9.
REF 174Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.
REF 175Biarylcarbamoylindolines 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 176SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
REF 177Serotonergic (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 1785-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 179Clinical pipeline report, company report or official report of Tonix Pharmaceuticals.
REF 180Autoradiographic 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 181Visualisation 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 182Autoradiographic 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 1837-[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 184Pharmacological characteristics of ATI-9242, a Novel Atypical Antipsychotic. FASEB J, April, 2010, 24(Meeting Abstract Supplement),773.12.
REF 185Deramciclane, 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 186(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 1875-HT(2A) inverse-agonists for the treatment of insomnia. Curr Top Med Chem. 2008;8(11):969-76.
REF 188Effects 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 189Modeling 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 190Clinical pipeline report, company report or official report of Lundbeck.
REF 191Bi-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.

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