Therapeutic Targets Database
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TTD Target ID: TTDS00103

Target Information
Name5-hydroxytryptamine 2A receptor    
Type of targetSuccessful target    
Synonyms5-HT-2    
5-HT-2A    
5-HT2A receptor    
5-hydroxytryptamine receptor 2A    
Serotonin receptor    
Serotonin receptor 2A    
DiseaseAcute ureteric colic
[ICD9: 788.0   ICD10: N23]
[1]
Anxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[2]
Arterial embolism and thrombosis
[ICD9: 437.6, 444.9, 453, 671.5, 671.9   ICD10: I74, I80-I82, I82, O88, T79.0-T79.1]
[3]
Cocaine dependence
[ICD9: 304.2   ICD10: F14.2]
[4]
Depression
[ICD9: 311   ICD10: F32]
[2]
Diabetic nephropathy
[ICD9: 250.4   ICD10: E10.2, E11.2, E13.2]
[5]
Diabetic neuropathy
[ICD9: 250.6   ICD10: E10.4, E11.4, E13.4]
[5]
Essential (primary) hypertension
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
[6]
Migraine
[ICD9: 346   ICD10: G43]
[7]
Schizophrenia
[ICD9: 295   ICD10: F20]
[2]
Drug(s)AsenapineApprovedSchizophrenia and bipolar disorder[8][9]
IloperidoneApprovedSchizophrenia[8][10]
SarpogrelateApprovedDiabetes mellitus[11][12][12][5]
Risperidone ConstaPhase IVBipolar disorder[9]
Lurasidone hydrochloridePhase III completedSchizophrenia[10]
SR46349BPhase III completedSleep Initiation and Maintenance Disorders; Primary Insomnia; Schizophrenia[10]
BlonanserinPhase IIISchizophrenia[10]
FlibanserinPhase IIIFemale sexual dysfunction[13]
PimavanserinPhase IIIParkinson's Disease Psychosis[14][15][16]
OcaperidonePhase IISchizophrenia[10]
TGBA01ADPhase IISevere Mood Disorders[17]
1192U90DiscontinuedSchizophrenia[10]
AdatanserinDiscontinued in Phase IISevere Mood Disorders[17][18]
FananserinDiscontinuedSchizophrenia[10]
LY367265DiscontinuedDepression[19]
YM-992Discontinued in Phase IIDepression[19]
Abaperidone hydrochlorideNo development reportedSchizophrenia[10]
GMC-283No development reportedSchizophrenia[10]
Org-23366No development reportedSchizophrenia[10]
ZD-3638No development reportedSchizophrenia[10]
Org-23366PreclinicalSchizophrenia[10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Gap junction
Neuroactive ligand-receptor interaction
UniProt IDP28223
FunctionThis is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins.    
SequenceMDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
Related US Patent6,143,792
6,316,468
6,576,670
6,638,934
6,664,274
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[20]
5-MEO-DMT[21]
5-METHOXYTRYPTAMINE[22]
6-bromoaplysinopsin[23]
A-80426[24]
A-987306[25]
ALTANSERIN[26]
APLYSINOPSIN[27]
Aniracetam[28]
BARETTIN[29]
Brolamfetamine[30]
CHLOROPHENYLPIPERAZINE[31]
CINANSERIN[22]
DOM[32]
Dimethyltryptamine[33]
EMD-281014[34]
Etisulergine[35]
FLUANISONE[36]
GR-127935[37]
ISOCLOZAPINE[38]
L-745870[39]
LY367265[19]
LY433222[19]
LYSERGIC ACID DIETHYLAMIDE[40]
MAZAPERTINE[41]
MDL-11939[42]
MDL-28161[42]
MESCALINE[32]
N-3'-ethylaplysinopsin[23]
NELOTANSERIN[43]
PG-01037[44]
PHENETHYLAMINE[45]
PHENYLPIPERAZINE[46]
PRUVANSERIN[43]
PSILOCIN[32]
QUIPAZINE[47]
RP-68303[48]
Racemic DOI[32]
Racemic DOTFM[32]
Ro-60-0175,   Ro-600175[49]
SB-243213[50]
SB-271046[51]
SEROTONIN[47]
SPIPERONE[52]
TIOSPIRONE[53]
TRYPTAMINE[22]
TRYPTOLINE[54]
VER-2692[55]
VER-3323[56]
VER-5384[56]
VER-5593[56]
VOLINANSERIN[26]
WAY-208466[57]
YM-348[58]
YM-992[19]
ZOTEPINE[59]
AgonistDV-7028[60][3][61]
Flibanserin[13]
MMDA[62]
TGBA01AD[17]
Antagonist1192U90[10]
Abaperidone hydrochloride[10]
Adatanserin[17][18]
Asenapine[8][9]
Blonanserin[10]
Fananserin[10]
GMC-283[10]
Iloperidone[8][10]
LY53857[63][64][65][66]
Lurasidone hydrochloride[10]
M100907[4]
Ocaperidone[10]
Org-23366[10]
Pimavanserin[14][15][16]
Risperidone Consta[9]
Ritanserin[67][68][66]
Sarpogrelate[11][12][12][5]
BinderSR46349B[10]
ZD-3638[10]
Multitarget1192U90[10]
Abaperidone hydrochloride[10]
Adatanserin[17][18]
Asenapine[8][9]
Blonanserin[10]
Flibanserin[13]
GMC-283[10]
Iloperidone[8][10]
Lurasidone hydrochloride[10]
Ocaperidone[10]
Org-23366[10]
Risperidone Consta[9]
SR46349B[10]
TGBA01AD[17]
ZD-3638[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 5Therapeutic effect of sarpogrelate, a new 5-hydroxytryptamine receptor 2A antagonist, on diabetic nephropathy and neuropathy. Nephron. 1997;76(2):227-9. To Reference
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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