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 Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
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]
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]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
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
Ref 522405ClinicalTrials.gov (NCT00735683) A Short-Term Study to Examine the Effects of ATHX-105 Phosphate on Weight Loss and Safety. U.S. National Institutes of Health.
Ref 522459ClinicalTrials.gov (NCT00768612) Study Evaluating Safety and Tolerability of Vabicaserin in Patients With Sudden Worsening of Schizophrenia. U.S. National Institutes of Health.
Ref 522480ClinicalTrials.gov (NCT00788515) Comparison of Volinanserin and Lormetazepam in the Treatment of Insomnia Characterized by Sleep Maintenance Difficulties. U.S. National Institutes of Health.
Ref 522602ClinicalTrials.gov (NCT00854724) Puerarin Effects on Alcohol Drinking. U.S. National Institutes of Health.
Ref 523309ClinicalTrials.gov (NCT01266174) Effects of Eltoprazine on Cognitive Impairment Associated With Schizophrenia (CIAS) in Adults. U.S. National Institutes of Health.
Ref 525381Dopaminergic mechanisms of reinstatement of MDMA-seeking behaviour in rats. Br J Pharmacol. 2011 Apr;162(8):1770-80.
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 536306Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536710Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
Ref 537244Local effect of tramadol on formalin evoked flinching behavior in rats. Rev Bras Anestesiol. 2008 Jul-Aug;58(4):375-9, 371-5.
Ref 538459FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012516.
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)
Ref 546467Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008324)
Ref 546616Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009204)
Ref 547441Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016366)
Ref 547560Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017316)
Ref 548243Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023694)
Ref 5515522011 Pipeline of Proximagen Group plc.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525458Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.
Ref 525477High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action. J Neurochem. 1999 May;72(5):2127-34.
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.
Ref 5257222-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem. 2000 Mar 9;43(5):1011-8.
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.
Ref 525929Evidence 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 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.
Ref 526713J 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 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.
Ref 526978mCPP-induced hyperactivity in 5-HT2C receptor mutant mice is mediated by activation of multiple 5-HT receptor subtypes. Neuropharmacology. 2004 Apr;46(5):663-71.
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.
Ref 528502Anxiolytic activity of a novel potent serotonin 5-HT2C receptor antagonist FR260010: a comparison with diazepam and buspirone. Eur J Pharmacol. 2006 Dec 28;553(1-3):171-84. Epub 2006 Sep 28.
Ref 528690Bioorg 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 528974J 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 529148Bioorg 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 529168Bioorg 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 529191Bioorg 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 529221Bioorg 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 529582Bioorg 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.
Ref 529789J 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 530209Bioorg 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 530516Bioorg 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 530558Bioorg 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 530589Bioorg 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 530936Bioorg 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.
Ref 531079J 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 531171J 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 |A(1)-adrenoceptors.
Ref 531390Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. J Pharmacol Exp Ther. 2011 Jun;337(3):673-80.
Ref 534232A novel class of 5-HT2A receptor antagonists: aryl aminoguanidines. Life Sci. 1996;59(15):1259-68.
Ref 534428SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
Ref 534475SB-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 534609Deramciclane, 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 534693Antiaversive effects of 5HT2C receptor agonists and fluoxetine in a model of panic-like anxiety in rats. Eur Neuropsychopharmacol. 1998 Aug;8(3):161-8.
Ref 535230SB-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.
Ref 535896The fenfluramine metabolite (+)-norfenfluramine is vasoactive. J Pharmacol Exp Ther. 2004 May;309(2):845-52. Epub 2004 Jan 29.
Ref 535927Some studies on the 5-hydroxytryptamine receptors in the isolated rat uterus. Afr J Med Med Sci. 2002 Dec;31(4):361-5.
Ref 536044Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82.
Ref 536175Serotonin 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.
Ref 536286Serotonin 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 536315Serotonergic 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.
Ref 536352The 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 536392Intake of fermented soybean (natto) increased locomotor activity in mice. Biol Pharm Bull. 2007 Apr;30(4):845-6.
Ref 536571Inverse 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.
Ref 536656Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice. Behav Pharmacol. 2008 Mar;19(2):145-52.
Ref 536679Spinal 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.
Ref 536710Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
Ref 536734Hypersensitivity 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.
Ref 536787Characterization 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 537068Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
Ref 538142p-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 543963(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: 8).
Ref 544074Pharmacological targeting of the serotonergic system for the treatment of obesity. J Physiol. 2009 January 1; 587(Pt 1): 49-60.
Ref 547442Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016366)
Ref 550266Clinical pipeline report, company report or official report of Arena Pharmaceuticals (2011).
Ref 551057Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
Ref 551219Synthesis 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 551382The 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 5515522011 Pipeline of Proximagen Group plc.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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