Therapeutic Targets Database
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TTD Target ID: TTDS00105

Target Information
Name5-hydroxytryptamine 2C receptor    
Type of targetSuccessful target    
Synonyms5-HT-2C    
5-HT2C receptor    
5HT-1C    
Serotonin receptor    
Serotonin receptor 2C    
DiseaseAcute ureteric colic    [1]
Cocaine dependence    [2]
Motor disorder    [3]
Schizophrenia    [3]
Drug(s)MethysergideApprovedMigraine headaches[4][5][6][7]
MirtazapineApprovedDepression[8][9]
NefazodoneApprovedDepression[9][10]
LorcaserinPhase III completedObesity[11][12]
SR46349BPhase III completedSleep Initiation and Maintenance Disorders; Primary Insomnia; Schizophrenia[13]
PRX00933Phase IIObesity, diabetes[14]
LorcaserinPhase I completedDrug Abuse[11][12]
5-HT2C agonistPreclinicalSchizophrenia[13]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Gap junction
Neuroactive ligand-receptor interaction
UniProt IDP28335
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.    
SequenceMVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Related US Patent6,433,175
6,576,670
6,638,934
6,638,936
6,638,953
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[15]
(2S)-1-[16]
(2S)-1-[16]
(2S)-1-[16]
(2S)-1-[16]
(E)-2-[17]
(R,S)-1-[18]
(R,S)-1-[18]
(R,S)-1-[18]
(R,S)-1-[18]
(R,S)-1-[18]
(S)-1-[18]
1- ([19]
1- ([19]
1- ([19]
1- ([19]
1- ([19]
1- ([19]
1- (2-Dimethylamino-ethyl)-1H-indol-4-ol[20]
1- (2-aminoethyl)-1H-indazol-6-ol[19]
1- (piperazin-1-yl)isoquinoline[21]
1-Butyl-3- (2-dimethylamino-ethyl)-1H-indol-4-ol[20]
2- (piperazin-1-yl)-5,6,7,8-tetrahydroquinoline[21]
3- (2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol[20]
3- (2-Dimethylamino-ethyl)-1H-indol-6-ol[20]
3- (2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol[20]
3- (2-Dimethylamino-propyl)-1H-indol-4-ol[20]
3- (2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol[20]
3- (3-Dimethylamino-propyl)-1H-indol-4-ol[20]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol[20]
3-Dimethylaminomethyl-1H-indol-4-ol[20]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[22]
4- (piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine[21]
4- (piperazin-1-yl)furo[3,2-c]pyridine[21]
4- (piperazin-1-yl)thieno[2,3-d]pyrimidine[21]
4- (piperazin-1-yl)thieno[3,2-c]pyridine[21]
4- (piperazin-1-yl)thieno[3,2-d]pyrimidine[21]
5,6-dichloro-3,4-dihydroquinazolin-2-amine[23]
5-MEO-DMT[19]
5-chloro-3,4-dihydroquinazolin-2-amine[23]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine[23]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine[23]
5-chloro-N- (pyridin-3-yl)indoline-1-carboxamide[18]
5-hydroxy-alpha-methyltryptamine[19]
5-methoxy-alpha-methyltryptamine[19]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine[24]
6- (piperazin-1-yl)-9-propyl-9H-purine[21]
6-bromo-2'-de-N-methylaplysinopsin[25]
6-bromo-8- (piperazin-1-yl)imidazo[1,2-a]pyrazine[21]
6-bromoaplysinopsin[25]
6-chloro-N- (pyridin-3-yl)indoline-1-carboxamide[18]
6-methyl-4- (piperazin-1-yl)furo[2,3-d]pyrimidine[21]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine[24]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine[24]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine[23]
APLYSINOPSIN[18]
BARETTIN[26]
CHLOROPHENYLPIPERAZINE[27]
EMD-281014[28]
GR-127935[29]
N- (6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide[30]
N- (pyridin-3-yl)indoline-1-carboxamide[18]
N-3'-ethylaplysinopsin[25]
NELOTANSERIN[31]
OCTOCLOTHEPIN[32]
PG-01037[33]
PRUVANSERIN[31]
RS-102,221[34]
Ro-60-0175,   Ro-600175[16]
SB-243213[30]
SB-271046[35]
SEROTONIN[26]
VER-2692[36]
VER-3323[37]
VER-5384[37]
VER-5593[37]
VOLINANSERIN[38]
WAY-181187[39]
WAY-208466[40]
WAY-466[41]
YM-348[24]
[2- (4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine[20]
cyclo[ (6-bromotryptophan)arginine][26]
Agonist3,4-Methylenedioxymethamphetamine[42]
5-HT2C agonist[13]
Lorcaserin[11][12]
PRX00933[14]
SB 243213[3]
AntagonistBVT 933[43]
LY53857[44][45][46][7]
Methysergide[4][5][6][7]
Mirtazapine[8][9]
Nefazodone[9][10]
Ritanserin[47][48][49][50]
SB 206553 hydrochloride[51][52]
BinderSR46349B[13]
MultitargetSR46349B[13]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2Enhanced locomotor, reinforcing, and neurochemical effects of cocaine in serotonin 5-hydroxytryptamine 2C receptor mutant mice. J Neurosci. 2002 Nov 15;22(22):10039-45. To Reference
Ref 3SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99. To Reference
Ref 4Spinal serotonin receptor activation modulates the exercise ventilatory response with increased dead space in goats. Respir Physiol Neurobiol. 2008 May 31;161(3):230-8. Epub 2008 Feb 29. To Reference
Ref 5Intake of fermented soybean (natto) increased locomotor activity in mice. Biol Pharm Bull. 2007 Apr;30(4):845-6. To Reference
Ref 6Serotonergic mechanisms of the lateral parabrachial nucleus in renal and hormonal responses to isotonic blood volume expansion. Am J Physiol Regul Integr Comp Physiol. 2007 Mar;292(3):R1190-7. Epub 2006 Nov 30. To Reference
Ref 7p-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. To Reference
Ref 8Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulation of cell surface expression and signal transduction. Mol Pharmacol. 2008 Mar;73(3):748-57. Epub 2007 Dec 14. To Reference
Ref 9Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60. To Reference
Ref 10Curr Top Med Chem. 2006;6(17):1801-23.Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. To Reference
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Ref 15Bioorg 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. To Reference
Ref 16Bioorg 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. To Reference
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Ref 21Bioorg 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. To Reference
Ref 22J 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. To Reference
Ref 23Bioorg 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. To Reference
Ref 24Bioorg 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. To Reference
Ref 25J 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. To Reference
Ref 26J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. To Reference
Ref 27Bioorg 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. To Reference
Ref 28Bioorg Med Chem Lett. 2006 Jun 15;16(12):3201-4. Epub 2006 May 2.A new class of selective, non-basic 5-HT2A receptor antagonists. To Reference
Ref 29Bioorg Med Chem Lett. 2005 Nov 1;15(21):4786-9.Synthesis of potent and selective serotonin 5-HT1B receptor ligands. To Reference
Ref 30Bioorg Med Chem Lett. 2008 Jul 15;18(14):3844-7. Epub 2008 Jun 21.Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: a novel series of 5-HT2C receptor antagonists. To Reference
Ref 31J Med Chem. 2010 Aug 12;53(15):5696-706.Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia. To Reference
Ref 32J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for ¦Á(1)-adrenoceptors. To Reference
Ref 33J 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. To Reference
Ref 34J 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. To Reference
Ref 35Bioorg 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. To Reference
Ref 36Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. To Reference
Ref 37Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists. To Reference
Ref 38Bioorg Med Chem Lett. 2010 Jun 15;20(12):3708-12. Epub 2010 Apr 24.Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders. To Reference
Ref 39J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist. To Reference
Ref 40Bioorg 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. To Reference
Ref 41J Med Chem. 2005 Jan 27;48(2):353-6.Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. To Reference
Ref 42Freudenmann RW, Oxler F, Bernschneider-Reif S: The origin of MDMA (ecstasy) revisited: the true story reconstructed from the original documents. Addiction. 2006 Sep;101(9):1241-5. To Reference
Ref 43Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. To Reference
Ref 44The 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. To Reference
Ref 45Some studies on the 5-hydroxytryptamine receptors in the isolated rat uterus. Afr J Med Med Sci. 2002 Dec;31(4):361-5. To Reference
Ref 46The fenfluramine metabolite (+)-norfenfluramine is vasoactive. J Pharmacol Exp Ther. 2004 May;309(2):845-52. Epub 2004 Jan 29. To Reference
Ref 47Characterization 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. To Reference
Ref 48Hypersensitivity of 5-HT2 receptors in OCD patients. An increased prolactin response after a challenge with meta-chlorophenylpiperazine and pre-treatment with ritanserin and placebo. J Psychiatr Res. 2008 Sep;42(11):894-901. Epub 2008 Jun 3. To Reference
Ref 49Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice. Behav Pharmacol. 2008 Mar;19(2):145-52. To Reference
Ref 50Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82. To Reference
Ref 51Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex. Neuropsychopharmacology. 2006 Feb;31(2):265-77. To Reference
Ref 52Strain-dependent effects of diazepam and the 5-HT2B/2C receptor antagonist SB 206553 in spontaneously hypertensive and Lewis rats tested in the elevated plus-maze. Braz J Med Biol Res. 2001 May;34(5):675-82. To Reference



 

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