Target General Infomation
Target ID
T31204
Former ID
TTDS00104
Target Name
5-hydroxytryptamine 2B receptor
Gene Name
HTR2B
Synonyms
5-HT 2B; 5-HT-2B; Serotonin receptor; Serotonin receptor 2B; HTR2B
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Congestive heart failure [ICD9: 428; ICD10: I50]
Coronary heart disease [ICD9: 414; ICD10: I25.1]
Depression; Cerebral infarction [ICD9:311; ICD10: F30-F39, I63]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Migraine [ICD9: 346; ICD10: G43]
Pulmonary arterial hypertension [ICD9: 416; ICD10: I27.0, I27.2]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Psychoses [ICD9: 290-299; ICD10: F20-F29]
Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. 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. Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5- hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain. Plays a role in the regulation of behavior, including impulsive behavior. Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine.
BioChemical Class
GPCR rhodopsin
Target Validation
T31204
UniProt ID
Sequence
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL
ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM
WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW
LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT
IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET
LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM
LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY
V
Drugs and Mode of Action
Drug(s) Minaprine Drug Info Approved Depression; Cerebral infarction [536164], [551871]
Triflupromazine Drug Info Approved Psychoses [467669], [538443]
PRX-08066 Drug Info Phase 2 Pulmonary arterial hypertension [536294]
Vabicaserin Drug Info Phase 2 Psychotic disorders [522459]
FENDILINE Drug Info Withdrawn from market Coronary heart disease [533443]
Ritanserin Drug Info Discontinued in Phase 3 Anxiety disorder [543335], [544590]
MT-500 Drug Info Discontinued in Phase 1 Migraine [547201]
LY53857 Drug Info Terminated Discovery agent [539138], [544876]
Ro-60-0175 Drug Info Terminated Discovery agent [539026], [546467]
SB 206553 Drug Info Terminated Discovery agent [539189], [546078]
Agonist (+)-LSD Drug Info [527178]
(+)-norfenfluramine Drug Info [525929]
(-)-norfenfluramine Drug Info [525929]
2-methyl-5-HT Drug Info [534042]
3,4-Methylenedioxymethamphetamine Drug Info [551382]
5-CT Drug Info [534042]
AL-37350A Drug Info [526713]
alpha-methyl-5-HT Drug Info [527238]
BRL-15572 Drug Info [534475]
BW723C86 Drug Info [526719]
dihydroergocryptine Drug Info [532279]
m-chlorophenylpiperazine Drug Info [534042]
norfenfluramine Drug Info [525929]
Org 12962 Drug Info [527178]
SB 216641 Drug Info [534475]
TFMPP Drug Info [534042]
[125I]DOI Drug Info [543921]
[3H]5-HT Drug Info [534042]
[3H]LSD Drug Info [526621]
Inhibitor (+/-)-nantenine Drug Info [530558]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info [527952]
(5-methoxy-1H-indol-3-yl)methanamine Drug Info [531223]
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-(3-(pentafluorosulfanyl)phenyl)propan-2-amine Drug Info [529013]
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]
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-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]
5-MEO-DMT Drug Info [527952]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info [529221]
6-Fluoromelatonin Drug Info [531223]
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]
A-987306 Drug Info [529789]
ADRENOGLOMERULOTROPIN Drug Info [531223]
ADS-103253 Drug Info [528581]
ADS-103274 Drug Info [528581]
CHLOROPHENYLPIPERAZINE Drug Info [530589]
FENDILINE Drug Info [531223]
Racemic DOI Drug Info [529789]
Ro-60-0175 Drug Info [527833]
SEROTONIN Drug Info [527833]
VER-2692 Drug Info [527833]
VER-3323 Drug Info [527037]
VER-5384 Drug Info [527037]
VER-5593 Drug Info [527037]
YM-348 Drug Info [529221]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info [527668]
Antagonist 1-naphthylpiperazine Drug Info [534042]
EGIS-7625 Drug Info [527053]
LY53857 Drug Info [538142]
LY86057 Drug Info [534042]
metergoline Drug Info [527178]
Minaprine Drug Info [535814], [536549]
MT-500 Drug Info [551871]
norfluoxetine Drug Info [525929]
piribedil Drug Info [526443]
PRX-08066 Drug Info [536294]
R-1 Drug Info [543921]
Ritanserin Drug Info [538142]
RQ-00310941 Drug Info [543921]
SB 204741 Drug Info [527178]
SB 206553 Drug Info [535165]
SB 215505 Drug Info [525458]
SB 221284 Drug Info [527178]
SB 228357 Drug Info [525730]
SB 242084 Drug Info [534428]
Small molecule 33 Drug Info [543921]
spiramide Drug Info [527178]
spiroxatrine Drug Info [534554]
Triflupromazine Drug Info [537770]
[3H]mesulergine Drug Info [527178]
[3H]rauwolscine Drug Info [534554]
Modulator 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 467669(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: 4330).
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 533443Value of fendiline in the treatment of patients with stable angina pectoris. Pol Tyg Lek. 1987 Nov 16;42(46):1456-8.
Ref 536164Novel cholinesterase inhibitors as future effective drugs for the treatment of Alzheimer's disease. Expert Opin Investig Drugs. 2006 Jan;15(1):1-12.
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 538443FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011123.
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 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 539189(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: 189).
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 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 546078Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006211)
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 547201Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013923)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525458Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.
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 526443Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804.
Ref 526621Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci. 2003 May 30;73(2):193-207.
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 527037Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists.
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 527238The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. Epub 2004 Oct 4.
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 528581Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists.
Ref 529013Bioorg Med Chem. 2007 Nov 1;15(21):6659-66. Epub 2007 Aug 15.The synthesis and biological activity of pentafluorosulfanyl analogs of fluoxetine, fenfluramine, and norfenfluramine.
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 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 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 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 531223J Med Chem. 2010 Nov 11;53(21):7573-86.Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs.
Ref 531390Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. J Pharmacol Exp Ther. 2011 Jun;337(3):673-80.
Ref 532279Structural features for functional selectivity at serotonin receptors. Science. 2013 May 3;340(6132):615-9.
Ref 534042Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. Mol Pharmacol. 1993 Mar;43(3):419-26.
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 534554[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24.
Ref 535165Strain-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.
Ref 535814Protective effect of minaprine against the abnormal changes of 2-deoxyglucose uptake by rat hippocampal slices induced by hypoxia/hypoglycemia. Jpn J Pharmacol. 1992 Sep;60(1):33-8.
Ref 536294Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
Ref 536549Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
Ref 537770Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85.
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 543921(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: 7).
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 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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