Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

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
[ICD9: 788.0   ICD10: N23]
[1]
Cocaine dependence
[ICD9: 304.2   ICD10: F14.2]
[2]
Motor disorder[3]
Schizophrenia
[ICD9: 295   ICD10: F20]
[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
Ref 1Effects of ketanserin and DOI on spontaneous and 5-HT-evoked peristalsis of the pig ureter in vivo. Br J Pharmacol. 2002 Feb;135(4):1026-32. To Reference
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
Ref 11Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50. To Reference
Ref 122011 Pipeline of Arena Pharmaceuticals. To Reference
Ref 13The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 142011 Pipeline of Proximagen Group plc. To Reference
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
Ref 17Bioorg 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. To Reference
Ref 18Bioorg. Med. Chem. 18(13):4783-4792 (2010) To Reference
Ref 19J 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. To Reference
Ref 20Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist. To Reference
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 (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



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543