5-HT2B receptor

5-hydroxytryptamine (serotonin) receptor 2B, also known as HTR2B, is a 5-HT₂ receptor, but also denotes the human gene encoding it.cite web | title = Entrez Gene: HTR_2B 5-hydroxytryptamine (serotonin) receptor 2B| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3357| accessdate = ] cite journal | author = Schmuck K, Ullmer C, Engels P, Lübbert H | title = Cloning and functional characterization of the human 5-HT_2B serotonin receptor | journal = FEBS Lett. | volume = 342 | issue = 1 | pages = 85–90 | year = 1994 | month = March | pmid = 8143856 | doi = | url = http://linkinghub.elsevier.com/retrieve/pii/0014-5793(94)80590-3 | issn = ]

Function

The 5-HT₂ receptors (of which the 5-HT_2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system effects include neuronal sensitization to tactile stimuli and mediation of hallucinogenic effects of phenylisopropylamine hallucinogens.

The 5-HT_2B receptor subtype is involved in:
* CNS: presynaptic inhibition, behavioural effectscite journal | author = Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L | title = Serotonin 5-HT_2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro | journal = J. Neurosci. | volume = 28 | issue = 11 | pages = 2933–40 | year = 2008 | month = March | pmid = 18337424 | doi = 10.1523/JNEUROSCI.5723-07.2008 | url = | issn = ]
* vascular: pulmonary vasoconstrictioncite journal | author = Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L | title = Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension | journal = Nat. Med. | volume = 8 | issue = 10 | pages = 1129–35 | year = 2002 | month = October | pmid = 12244304 | doi = 10.1038/nm764 | url = | issn = ]

Ligands

As of 2008, few highly selective 5-HT_2B receptor ligands have been discovered. However, numerous potent non-selective compounds are known, particularly agents with concomitant 5-HT_2C binding. An overview was published in 2007.cite paper | author = Schuhmacher M | title = [Chiral arylmethoxytryptamines as 5-HT_2B-receptor antagonists: synthesis, analysis and in-vitro pharmacology] (German) | version = Ph.D. Dissertation | publisher = University of Regensburg | date = 2007 | pages = pages 6-17 | url = http://www.opus-bayern.de/uni-regensburg/volltexte/2008/796/pdf/Dissertation_Schumacher.pdf | accessdate = 2008-08-11 ]

Agonists

* BW-723C86:cite journal |author=Porter RH, Benwell KR, Lamb H, "et al" |title=Functional characterization of agonists at recombinant human 5-HT_2A, 5-HT_2B and 5-HT_2C receptors in CHO-K1 cells |journal=Br. J. Pharmacol. |volume=128 |issue=1 |pages=13–20 |year=1999 |pmid=10498829 |pmc=1571597 |doi=10.1038/sj.bjp.0702751 |url=] fair functional subtype selectivity; almost full agonist
* Ro 60-0175: functionally selective over 5-HT_2A, moderately over 5-HT_2C; almost full agonist
* Pergolidecite journal |author=Görnemann T, Hübner H, Gmeiner P, "et al" |title=Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine_2B and 5-Hydroxytryptamine_2A receptors |journal=J. Pharmacol. Exp. Ther. |volume=324 |issue=3 |pages=1136–45 |year=2008 |pmid=18096760 |doi=10.1124/jpet.107.133165 |url=] and nor-dexfenfluramine (both non-selective)

Antagonists

* RS-127445:cite journal |author=Bonhaus DW, Flippin LA, Greenhouse RJ, "et al" |title=RS-127445: a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist |journal=Br. J. Pharmacol. |volume=127 |issue=5 |pages=1075–82 |year=1999 |pmid=10455251 |pmc=1566110 |doi=10.1038/sj.bjp.0702632 |url=] high affinity; subtype selective (1000x), selective over at least eight other 5-HTR types; orally bioavailable.
* SB-204,741 (N-(1-Methyl-1H-indolyl-5-yl)-N-(3-methyl-5-isothiazolyl)urea)
* SB-215,505 (6-chloro-5-methyl-1-(5-quinolylcarbamoyl)indoline)

ee also

* 5-HT receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Raymond JR, Mukhin YV, Gelasco A, "et al." |title=Multiplicity of mechanisms of serotonin receptor signal transduction. |journal=Pharmacol. Ther. |volume=92 |issue= 2-3 |pages= 179–212 |year= 2002 |pmid= 11916537 |doi=
*cite journal | author=Bonhaus DW, Bach C, DeSouza A, "et al." |title=The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. |journal=Br. J. Pharmacol. |volume=115 |issue= 4 |pages= 622–8 |year= 1995 |pmid= 7582481 |doi=
*cite journal | author=Choi DS, Birraux G, Launay JM, Maroteaux L |title=The human serotonin 5-HT2B receptor: pharmacological link between 5-HT2 and 5-HT1D receptors. |journal=FEBS Lett. |volume=352 |issue= 3 |pages= 393–9 |year= 1994 |pmid= 7926008 |doi=
*cite journal | author=Kursar JD, Nelson DL, Wainscott DB, Baez M |title=Molecular cloning, functional expression, and mRNA tissue distribution of the human 5-hydroxytryptamine2B receptor. |journal=Mol. Pharmacol. |volume=46 |issue= 2 |pages= 227–34 |year= 1994 |pmid= 8078486 |doi=
*cite journal | author=Schmuck K, Ullmer C, Engels P, Lübbert H |title=Cloning and functional characterization of the human 5-HT2B serotonin receptor. |journal=FEBS Lett. |volume=342 |issue= 1 |pages= 85–90 |year= 1994 |pmid= 8143856 |doi=
*cite journal | author=Launay JM, Birraux G, Bondoux D, "et al." |title=Ras involvement in signal transduction by the serotonin 5-HT2B receptor. |journal=J. Biol. Chem. |volume=271 |issue= 6 |pages= 3141–7 |year= 1996 |pmid= 8621713 |doi=
*cite journal | author=Le Coniat M, Choi DS, Maroteaux L, "et al." |title=The 5-HT2B receptor gene maps to 2q36.3-2q37.1. |journal=Genomics |volume=32 |issue= 1 |pages= 172–3 |year= 1996 |pmid= 8786115 |doi= 10.1006/geno.1996.0101
*cite journal | author=Kim SJ, Veenstra-VanderWeele J, Hanna GL, "et al." |title=Mutation screening of human 5-HT(2B)receptor gene in early-onset obsessive-compulsive disorder. |journal=Mol. Cell. Probes |volume=14 |issue= 1 |pages= 47–52 |year= 2000 |pmid= 10722792 |doi= 10.1006/mcpr.1999.0281
*cite journal | author=Manivet P, Mouillet-Richard S, Callebert J, "et al." |title=PDZ-dependent activation of nitric-oxide synthases by the serotonin 2B receptor. |journal=J. Biol. Chem. |volume=275 |issue= 13 |pages= 9324–31 |year= 2000 |pmid= 10734074 |doi=
*cite journal | author=Becamel C, Figge A, Poliak S, "et al." |title=Interaction of serotonin 5-hydroxytryptamine type 2C receptors with PDZ10 of the multi-PDZ domain protein MUPP1. |journal=J. Biol. Chem. |volume=276 |issue= 16 |pages= 12974–82 |year= 2001 |pmid= 11150294 |doi= 10.1074/jbc.M008089200
*cite journal | author=Manivet P, Schneider B, Smith JC, "et al." |title=The serotonin binding site of human and murine 5-HT2B receptors: molecular modeling and site-directed mutagenesis. |journal=J. Biol. Chem. |volume=277 |issue= 19 |pages= 17170–8 |year= 2002 |pmid= 11859080 |doi= 10.1074/jbc.M200195200
*cite journal | author=Borman RA, Tilford NS, Harmer DW, "et al." |title=5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro. |journal=Br. J. Pharmacol. |volume=135 |issue= 5 |pages= 1144–51 |year= 2002 |pmid= 11877320 |doi= 10.1038/sj.bjp.0704571
*cite journal | author=Strausberg RL, Feingold EA, Grouse LH, "et al." |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899–903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899
*cite journal | author=Matsuda A, Suzuki Y, Honda G, "et al." |title=Large-scale identification and characterization of human genes that activate NF-kappaB and MAPK signaling pathways. |journal=Oncogene |volume=22 |issue= 21 |pages= 3307–18 |year= 2003 |pmid= 12761501 |doi= 10.1038/sj.onc.1206406
*cite journal | author=Slominski A, Pisarchik A, Zbytek B, "et al." |title=Functional activity of serotoninergic and melatoninergic systems expressed in the skin. |journal=J. Cell. Physiol. |volume=196 |issue= 1 |pages= 144–53 |year= 2003 |pmid= 12767050 |doi= 10.1002/jcp.10287
*cite journal | author=Gerhard DS, Wagner L, Feingold EA, "et al." |title=The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). |journal=Genome Res. |volume=14 |issue= 10B |pages= 2121–7 |year= 2004 |pmid= 15489334 |doi= 10.1101/gr.2596504
*cite journal | author=Lin Z, Walther D, Yu XY, "et al." |title=The human serotonin receptor 2B: coding region polymorphisms and association with vulnerability to illegal drug abuse. |journal=Pharmacogenetics |volume=14 |issue= 12 |pages= 805–11 |year= 2005 |pmid= 15608559 |doi=
*cite journal | author=Hillier LW, Graves TA, Fulton RS, "et al." |title=Generation and annotation of the DNA sequences of human chromosomes 2 and 4. |journal=Nature |volume=434 |issue= 7034 |pages= 724–31 |year= 2005 |pmid= 15815621 |doi= 10.1038/nature03466

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