Target Information

Target General Infomation
Target ID
T83813
Former ID
TTDS00105
Target Name
5-hydroxytryptamine 2C receptor
Gene Name
HTR2C
Synonyms
5-HT-2C; 5-HT2C receptor; 5HT-1C; Serotonin receptor; Serotonin receptor 2C; HTR2C
Target Type
Successful
Disease Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Aggressive non-hodgkin's lymphoma [ICD9: 200, 201, 202, 202.8, 208.9; ICD10: C81, C81-C86, C82-C85, C91-C95]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Depression [ICD9: 311; ICD10: F30-F39]
Drug abuse [ICD9: 303-304; ICD10: F10-F19]
Generalized anxiety disorder; Major depressive disorder [ICD9:300, 300.02, 311, 296.2, 296.3, 710.0; ICD10: F32, F40-F42, F41.1, F33, M32]
Migraine headaches [ICD9: 346; ICD10: G43]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Mood disorder [ICD10: F30-F39]
Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Obesity [ICD9: 278; ICD10: E66]
Obesity; Diabetes [ICD9: 250, 278; ICD10: E08-E13, E66]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
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 for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 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 a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.
BioChemical Class
GPCR rhodopsin
Target Validation
T83813
UniProt ID
P28335
Sequence
MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Drugs and Mode of Action
Drug(s) Lorcaserin Drug Info Approved Obesity [532210], [539956]
Methysergide Drug Info Approved Migraine headaches [538459], [538818]
Mirtazapine Drug Info Approved Depression [536306], [542258]
Nefazodone Drug Info Approved Major depressive disorder [551871]
Tramadol Drug Info Approved Pain [537244], [543040]
SR46349B Drug Info Phase 3 Sleep initiation and maintenance disorders; Primary insomnia; Schizophrenia [536463]
VOLINANSERIN Drug Info Phase 3 Discovery agent [522480], [539159]
ATHX-105 Drug Info Phase 2 Obesity [522405]
Eltoprazine Drug Info Phase 2 Aggressive non-hodgkin's lymphoma [523309]
PRX00933 Drug Info Phase 2 Obesity; Diabetes [551552]
Puerarin Drug Info Phase 2 Alcohol use disorders [522602]
Vabicaserin Drug Info Phase 2 Psychotic disorders [522459]
Lorcaserin Drug Info Phase 1 Drug abuse [536710], [539956]
Tedatioxetine Drug Info Phase 1 Generalized anxiety disorder; Major depressive disorder [548243]
Nefazodone Drug Info Withdrawn from market Depression [536306], [542264]
Deramciclane Drug Info Discontinued in Phase 3 Anxiety disorder [540889], [544913]
Ritanserin Drug Info Discontinued in Phase 3 Anxiety disorder [543335], [544590]
MCPP Drug Info Discontinued in Phase 2 Mood disorder [525381]
R-1065 Drug Info Discontinued in Phase 1 Obesity [547560]
SB-247853 Drug Info Discontinued in Phase 1 Anxiety disorder [547441]
ICI-169369 Drug Info Terminated Anxiety disorder [539780], [544709]
LY53857 Drug Info Terminated Discovery agent [539138], [544876]
Org-37684 Drug Info Terminated Anxiety disorder [539062], [546616]
Ro-60-0175 Drug Info Terminated Discovery agent [539026], [546467]
SDZ-SER-082 Drug Info Terminated Neurological disease [539249], [546128]
Agonist (+)-LSD Drug Info [525477]
3,4-Methylenedioxymethamphetamine Drug Info [551382]
5-CT Drug Info [525661]
5-HT 2c receptor agonists (obesity/schizophrenia), Galenea Drug Info [543963]
5-HT2c agonists (metabolic disorders), Boehringer Drug Info [543963]
AL-37350A Drug Info [526713]
alpha-methyl-5-HT Drug Info [525477]
ATHX-105 Drug Info [544074]
BRL-15572 Drug Info [534475]
BW723C86 Drug Info [526719]
CP-809101 Drug Info [543963]
CSC-500297 Drug Info [543963]
Lorcaserin Drug Info [536710], [550266]
m-chlorophenylpiperazine Drug Info [526921]
MCPP Drug Info [526978], [551871]
Org 12962 Drug Info [527178]
Org-37684 Drug Info [526325]
PRX00933 Drug Info [551552]
R-1065 Drug Info [534693]
SB 216641 Drug Info [534475]
SB 243213 Drug Info [535230]
SB-247853 Drug Info [547442], [551871]
TFMPP Drug Info [525661]
TQ-1017 Drug Info [551871]
WAY-163909 Drug Info [527428]
[125I]DOI Drug Info [525477]
[3H]LSD Drug Info [543963]
Inhibitor (+/-)-nantenine Drug Info [530558]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info [529168]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [529168]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info [529168]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info [529168]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info [528690]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info [551219]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info [527952]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info [527952]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info [527952]
1-(2-Dimethylamino-ethyl)-1H-indol-4-ol Drug Info [527668]
1-(piperazin-1-yl)isoquinoline Drug Info [530516]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info [527668]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info [527952]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info [530516]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info [527952]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info [527668]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info [527668]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info [527668]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [527668]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info [527668]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info [527668]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info [527668]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info [527668]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Drug Info [530516]
4-(piperazin-1-yl)furo[3,2-c]pyridine Drug Info [530516]
4-(piperazin-1-yl)thieno[2,3-d]pyrimidine Drug Info [530516]
4-(piperazin-1-yl)thieno[3,2-c]pyridine Drug Info [530516]
4-(piperazin-1-yl)thieno[3,2-d]pyrimidine Drug Info [530516]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [529148]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [551219]
5-MEO-DMT Drug Info [527952]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info [529221]
6-(piperazin-1-yl)-9-propyl-9H-purine Drug Info [530516]
6-bromo-2'-de-N-methylaplysinopsin Drug Info [526321]
6-bromo-8-(piperazin-1-yl)imidazo[1,2-a]pyrazine Drug Info [530516]
6-bromoaplysinopsin Drug Info [526321]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [551219]
6-methyl-4-(piperazin-1-yl)furo[2,3-d]pyrimidine Drug Info [530516]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info [529221]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info [529221]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info [529148]
APLYSINOPSIN Drug Info [551219]
BARETTIN Drug Info [528498]
CHLOROPHENYLPIPERAZINE Drug Info [530589]
Cyclo[(6-bromotryptophan)arginine] Drug Info [528498]
N-(6-phenoxypyridin-3-yl)-1H-indole-3-carboxamide Drug Info [529582]
N-(pyridin-3-yl)indoline-1-carboxamide Drug Info [551219]
N-3'-ethylaplysinopsin Drug Info [526321]
OCTOCLOTHEPIN Drug Info [531171]
PG-01037 Drug Info [528974]
Ro-60-0175 Drug Info [529168]
RS-102,221 Drug Info [529789]
SB-271046 Drug Info [529191]
SEROTONIN Drug Info [528498]
VER-2692 Drug Info [527833]
VER-3323 Drug Info [527037]
VER-5384 Drug Info [527037]
VER-5593 Drug Info [527037]
VOLINANSERIN Drug Info [530936]
WAY-208466 Drug Info [530209]
WAY-466 Drug Info [527381]
YM-348 Drug Info [529221]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [527668]
Antagonist BVT 933 Drug Info [537068]
cyamemazine Drug Info [526510]
EGIS-7625 Drug Info [527053]
Eltoprazine Drug Info [551057]
FR260010 Drug Info [528502]
LY334362 Drug Info [534232]
LY53857 Drug Info [535896], [535927], [536352], [538142]
metergoline Drug Info [527178]
Methysergide Drug Info [536315], [536392], [536679], [538142]
Mirtazapine Drug Info [536175], [536571]
MPDT Drug Info [525722]
Nefazodone Drug Info [536175], [536286]
norfluoxetine Drug Info [525929]
Ritanserin Drug Info [536044], [536656], [536734], [536787]
SB 204741 Drug Info [527178]
SB 215505 Drug Info [525458]
SB 221284 Drug Info [527178]
SB 228357 Drug Info [525730]
SB 242084 Drug Info [534428]
spiramide Drug Info [527178]
[3H]mesulergine Drug Info [525477]
Modulator Deramciclane Drug Info [534609]
ICI-169369 Drug Info
MK-212 Drug Info
Puerarin Drug Info
SDZ-SER-082 Drug Info
SR46349B Drug Info
Tedatioxetine Drug Info [1572591]
Tramadol Drug Info [527050]
Vabicaserin Drug Info [531390]
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 ELK-SRF/GATA4 signaling
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
References
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Ref 538818(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: 134).
Ref 539026(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 539062(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: 171).
Ref 539138(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 539159(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 539249(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: 195).
Ref 539780(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 539956(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: 2941).
Ref 540889(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 542258(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: 7241).
Ref 542264(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: 7247).
Ref 543040(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: 8286).
Ref 543335(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 544590Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000237)
Ref 544709Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000690)
Ref 544876Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001395)
Ref 544913Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001479)
Ref 546128Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006463)
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Ref
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Ref 525661Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors. Synapse. 2000 Feb;35(2):144-50.
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Ref 525730Biarylcarbamoylindolines 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.
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Ref 526321J 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 526325Role of 5-hT2C receptors in the hypophagic effect of m-CPP, ORG 37684 and CP-94,253 in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Apr;26(3):441-9.
Ref 526510Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. Biochem Pharmacol. 2003 Feb 1;65(3):435-40.
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Ref 526719Agonist actions of dihydroergotamine at 5-HT2B and 5-HT2C receptors and their possible relevance to antimigraine efficacy. Br J Pharmacol. 2003 Sep;140(2):277-84. Epub 2003 Aug 11.
Ref 526921Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist. Eur J Pharmacol. 2004 Jan 1;483(1):37-43.
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Ref 527037Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
Ref 527050The inhibitory effects of tramadol on 5-hydroxytryptamine type 2C receptors expressed in Xenopus oocytes. Anesth Analg. 2004 May;98(5):1401-6, table of contents.
Ref 527053Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34.
Ref 527178Pharmacological 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 527381J 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.
Ref 527428WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a novel 5-hydroxytryptamine 2C receptor-selective agonist with anorectic activity. J Pharmacol Exp Ther. 2005 May;313(2):862-9. Epub 2005 Feb 10.
Ref 527668Bioorg Med Chem Lett. 2005 Oct 15;15(20):4555-9.SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Ref 527833Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. Epub 2005 Oct 27.Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Ref 527952J 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 528498J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
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