Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00104

Target Information
Name5-hydroxytryptamine 2B receptor    
Type of targetSuccessful target    
Synonyms5-HT 2B    
5-HT-2B    
Serotonin receptor    
Serotonin receptor 2B    
DiseaseAnxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[1]
Migraine
[ICD9: 346   ICD10: G43]
[2]
P-chloroamphetamine-induced hyperglycemia
[ICD9: 790.29   ICD10: R73.9]
[3]
Drug(s)MinaprineApprovedDepression[4][5]
TriflupromazineApprovedPsychoses[6]
PRX-08066Phase II completedPulmonary arterial hypertension[7]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Gap junction
Neuroactive ligand-receptor interaction
UniProt IDP41595
PDB Structure4IB4.    
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.    
SequenceMALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY V
Related US Patent6,444,477
6,638,953
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[8]
(+/-)DOI[9]
(5-methoxy-1H-indol-3-yl)methanamine[10]
(S)-2-[11]
1- ([11]
1- ([11]
1- ([11]
1- ([11]
1- ([11]
1- ([11]
1- (2-aminoethyl)-1H-indazol-6-ol[11]
1- (3-[12]
1-Butyl-3- (2-dimethylamino-ethyl)-1H-indol-4-ol[13]
3- (2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol[13]
3- (2-Dimethylamino-ethyl)-1H-indol-6-ol[13]
3- (2-Dimethylamino-propyl)-1H-indol-4-ol[13]
3- (2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol[13]
3- (3-Dimethylamino-propyl)-1H-indol-4-ol[13]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol[13]
3-Dimethylaminomethyl-1H-indol-4-ol[13]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[14]
5-MEO-DMT[11]
5-hydroxy-alpha-methyltryptamine[11]
5-methoxy-alpha-methyltryptamine[11]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine[15]
6-Fluoromelatonin[10]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine[15]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine[15]
A-987306[9]
ADRENOGLOMERULOTROPIN[10]
ADS-103253[16]
ADS-103274[16]
ATC-0175[17]
BP-897[10]
CHLOROPHENYLPIPERAZINE[18]
FENDILINE[10]
Ro-60-0175,   Ro-600175[19]
SB-206553[10]
SEROTONIN[19]
VER-2692[19]
VER-3323[20]
VER-5384[20]
VER-5593[20]
WAY-181187[21]
YM-348[15]
[2- (4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine[13]
Agonist3,4-Methylenedioxymethamphetamine[22]
AntagonistLY53857[3]
MT-500
Minaprine[4][5]
PRX-08066[7]
Ritanserin[3]
SB 206553[1]
Triflupromazine[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Strain-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
Ref 2Serotonin in migraine: theories, animal models and emerging therapies. Prog Drug Res. 1998;51:219-44. To Reference
Ref 3p-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 4Mini Rev Med Chem. 2007 Nov;7(11):1108-19.Privileged structures: a useful concept for the rational design of new lead drug candidates. To Reference
Ref 5Protective 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. To Reference
Ref 6Some properties of 5-hydroxytryptamine receptors in the hindquarters of the rat. Br J Pharmacol. 1979 Sep;67(1):79-85. To Reference
Ref 7Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. To Reference
Ref 8Bioorg 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 9J 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 10J 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. To Reference
Ref 11J 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 12Bioorg 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. To Reference
Ref 13Bioorg 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 14J 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 15Bioorg 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 16Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. Epub 2006 Dec 2.Quinazoline and benzimidazole MCH-1R antagonists. To Reference
Ref 17Bioorg Med Chem Lett. 2009 Nov 1;19(21):6166-71. Epub 2009 Sep 6.Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. To Reference
Ref 18Bioorg 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 19Bioorg 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 20Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70.Indoline derivatives as 5-HT(2C) receptor agonists. To Reference
Ref 21J 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 22Freudenmann 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



 

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