Просмотр кода страницы 5-HT2B-рецептор

{{DISPLAYTITLE:5-HT<sub>2B</sub>-рецептор}}

{{GNF_Protein_box
 | Name = 5-HT<sub>2B</sub>-рецептор
 | image = 4IB4.png
 | image_source = 
 | PDB = {{PDB2|4IB4}}, {{PDB2|4NC3}}
 | HGNCid = 5294
 | MGIid = 109323
 | Symbol = HTR2B
 | AltSymbols =; 5-HT(2B); 5-HT2B
 | IUPHAR = yes
 | ChEMBL = 1833
 | OMIM = 601122
 | ECnumber = 
 | Homologene = 55492
 | GeneAtlas_image1 = PBB_GE_HTR2B_206638_at_tn.png
 | GeneAtlas_image2 = 
 | GeneAtlas_image3 = 
 | Protein_domain_image = 
 | Function = {{GNF_GO|id=GO:0001965 |text = G-protein alpha-subunit binding}} {{GNF_GO|id=GO:0004993 |text = serotonin receptor activity}} {{GNF_GO|id=GO:0005099 |text = Ras GTPase activator activity}} {{GNF_GO|id=GO:0008144 |text = drug binding}} {{GNF_GO|id=GO:0051378 |text = serotonin binding}}
 | Component = {{GNF_GO|id=GO:0005737 |text = cytoplasm}} {{GNF_GO|id=GO:0005886 |text = plasma membrane}} {{GNF_GO|id=GO:0005887 |text = integral component of plasma membrane}} {{GNF_GO|id=GO:0030054 |text = cell junction}} {{GNF_GO|id=GO:0043005 |text = neuron projection}} {{GNF_GO|id=GO:0045202 |text = synapse}}
 | Process = {{GNF_GO|id=GO:0001755 |text = neural crest cell migration}} {{GNF_GO|id=GO:0001819 |text = positive regulation of cytokine production}} {{GNF_GO|id=GO:0001938 |text = positive regulation of endothelial cell proliferation}} {{GNF_GO|id=GO:0002031 |text = G-protein coupled receptor internalization}} {{GNF_GO|id=GO:0003007 |text = heart morphogenesis}} {{GNF_GO|id=GO:0003300 |text = cardiac muscle hypertrophy}} {{GNF_GO|id=GO:0006182 |text = cGMP biosynthetic process}} {{GNF_GO|id=GO:0006874 |text = cellular calcium ion homeostasis}} {{GNF_GO|id=GO:0007186 |text = G-protein coupled receptor signaling pathway}} {{GNF_GO|id=GO:0007202 |text = activation of phospholipase C activity}} {{GNF_GO|id=GO:0007205 |text = protein kinase C-activating G-protein coupled receptor signaling pathway}} {{GNF_GO|id=GO:0007210 |text = serotonin receptor signaling pathway}} {{GNF_GO|id=GO:0007610 |text = behavior}} {{GNF_GO|id=GO:0008284 |text = positive regulation of cell proliferation}} {{GNF_GO|id=GO:0010507 |text = negative regulation of autophagy}} {{GNF_GO|id=GO:0010513 |text = positive regulation of phosphatidylinositol biosynthetic process}} {{GNF_GO|id=GO:0014033 |text = neural crest cell differentiation}} {{GNF_GO|id=GO:0014065 |text = phosphatidylinositol 3-kinase signaling}} {{GNF_GO|id=GO:0014827 |text = intestine smooth muscle contraction}} {{GNF_GO|id=GO:0016310 |text = phosphorylation}} {{GNF_GO|id=GO:0019722 |text = calcium-mediated signaling}} {{GNF_GO|id=GO:0032320 |text = positive regulation of Ras GTPase activity}} {{GNF_GO|id=GO:0042310 |text = vasoconstriction}} {{GNF_GO|id=GO:0042493 |text = response to drug}} {{GNF_GO|id=GO:0043066 |text = negative regulation of apoptotic process}} {{GNF_GO|id=GO:0043123 |text = positive regulation of I-kappaB kinase/NF-kappaB signaling}} {{GNF_GO|id=GO:0043406 |text = positive regulation of MAP kinase activity}} {{GNF_GO|id=GO:0048598 |text = embryonic morphogenesis}} {{GNF_GO|id=GO:0050715 |text = positive regulation of cytokine secretion}} {{GNF_GO|id=GO:0050795 |text = regulation of behavior}} {{GNF_GO|id=GO:0051000 |text = positive regulation of nitric-oxide synthase activity}} {{GNF_GO|id=GO:0051209 |text = release of sequestered calcium ion into cytosol}} {{GNF_GO|id=GO:0051781 |text = positive regulation of cell division}} {{GNF_GO|id=GO:0060548 |text = negative regulation of cell death}} {{GNF_GO|id=GO:0070371 |text = ERK1 and ERK2 cascade}} {{GNF_GO|id=GO:0070374 |text = positive regulation of ERK1 and ERK2 cascade}} {{GNF_GO|id=GO:0070528 |text = protein kinase C signaling}} {{GNF_GO|id=GO:0071502 |text = cellular response to temperature stimulus}}
 | Hs_EntrezGene = 3357
 | Hs_Ensembl = ENSG00000135914
 | Hs_RefseqmRNA = NM_000867
 | Hs_RefseqProtein = NP_000858
 | Hs_GenLoc_db = hg19
 | Hs_GenLoc_chr = 2
 | Hs_GenLoc_start = 231972944
 | Hs_GenLoc_end = 231989832
 | Hs_Uniprot = P41595
 | Mm_EntrezGene = 15559
 | Mm_Ensembl = ENSMUSG00000026228
 | Mm_RefseqmRNA = NM_008311
 | Mm_RefseqProtein = NP_032337
 | Mm_GenLoc_db = mm10
 | Mm_GenLoc_chr = 1
 | Mm_GenLoc_start = 86099026
 | Mm_GenLoc_end = 86111970
 | Mm_Uniprot = Q02152
 | path = PBB/3357
}}

'''5-HT<sub>2B</sub>-рецептор''' — это [[белок]] одного из подтипов [[серотониновые рецепторы|серотониновых рецепторов]] подсемейства [[5-HT2-рецептор]]ов. У человека этот [[рецептор]]ный белок кодируется [[ген]]ом ''HTR2B''.<ref name="entrez_ 3357">{{cite web | title = Entrez Gene: HTR<sub>2B</sub> 5-hydroxytryptamine (serotonin) receptor 2B| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3357| accessdate = }}</ref><ref name="pmid8143856">{{cite journal | author = Schmuck K, Ullmer C, Engels P, Lübbert H | title = Cloning and functional characterization of the human 5-HT<sub>2B</sub> serotonin receptor | journal = FEBS Lett. | volume = 342 | issue = 1 | pages = 85–90 |date=March 1994 | pmid = 8143856 | doi = 10.1016/0014-5793(94)80590-3| url = http://linkinghub.elsevier.com/retrieve/pii/0014-5793(94)80590-3 }}</ref> Рецепторы подтипа 5-HT<sub>2B</sub> относятся к семейству метаботропных [[GPCR|G-белок-связанных]] рецепторов, и служат для связывания [[нейромедиатор]]а [[серотонин]]а (5-гидрокситриптамина, 5-HT).

== Функция ==

Рецепторы подсемейства 5-HT<sub>2</sub> (к которым относится и 5-HT<sub>2B</sub>-рецептор) опосредуют многие из [[центральная нервная система|центральных]] и периферических [[физиология|физиологических]] эффектов [[серотонин]]а у [[человек]]а и [[животное|животных]]. В частности, к [[сердечно-сосудистая система|сердечно-сосудистым]] эффектам активации 5-HT<sub>2B</sub>-рецепторов относится [[вазоконстрикция]] и изменения формы [[тромбоцит]]ов, а к [[центральная нервная система|центральным]] эффектам относится сенсибилизация [[нейрон]]ов к тактильным стимулам и опосредование некоторых эффектов [[галлюциноген]]ов, в частности замещённых [[амфетамин]]ов.

Рецепторы подтипа 5-HT<sub>2B</sub> вовлечены в:
* [[ЦНС]]: пресинаптическое ингибирование, поведенческие эффекты<ref name="pmid18337424">{{cite journal | author = Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L | title = Serotonin 5-HT<sub>2B</sub> 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 |date=March 2008 | pmid = 18337424 | doi = 10.1523/JNEUROSCI.5723-07.2008 | url =  }}</ref>
* [[Сосуды]]: [[лёгкие|лёгочная]] [[вазоконстрикция]]<ref name="pmid12244304">{{cite 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 |date=October 2002 | pmid = 12244304 | doi = 10.1038/nm764 | url =  }}</ref>
* [[Сердце]]: Рецепторы подтипа 5-HT<sub>2B</sub> регулируют структуру и функции сердечной мышцы, что иллюстрируется аномальным развитием сердца у [[мышь|мыши]], лишённой функционирующих 5-HT<sub>2B</sub> рецепторов.<ref name="pmid11413089">{{cite journal | author = Nebigil CG, Hickel P, Messaddeq N, Vonesch JL, Douchet MP, Monassier L, György K, Matz R, Andriantsitohaina R, Manivet P, Launay JM, Maroteaux L | title = Ablation of serotonin 5-HT(2B) receptors in mice leads to abnormal cardiac structure and function | journal = Circulation | volume = 103 | issue = 24 | pages = 2973–9 |date=June 2001 | pmid = 11413089 | doi = 10.1161/01.cir.103.24.2973| url = http://circ.ahajournals.org/cgi/content/abstract/103/24/2973 }}</ref> Стимуляция рецепторов подтипа 5-HT<sub>2B</sub> может также приводить к аномальной, патологической пролиферации фибробластов сердечных клапанов,<ref name="pmid18511249">{{cite journal | author = Elangbam CS, Job LE, Zadrozny LM, Barton JC, Yoon LW, Gates LD, Slocum N | title = 5-hydroxytryptamine (5HT)-induced valvulopathy: compositional valvular alterations are associated with 5HT2B receptor and 5HT transporter transcript changes in Sprague-Dawley rats | journal = Exp. Toxicol. Pathol. | volume = 60 | issue = 4–5 | pages = 253–62 |date=August 2008 | pmid = 18511249 | doi = 10.1016/j.etp.2008.03.005 | url =  }}</ref> что при хронической гиперстимуляции 5-HT<sub>2B</sub> может приводить к серьёзной вальвулопатии (клапанным порокам) и [[сердечная недостаточность|сердечной недостаточности]]. Более того, сравнительно недавно было показано, что рецепторы подтипа 5-HT<sub>2B</sub> гиперэкспрессированы в сердце людей, страдающих сердечной недостаточностью, и что антагонисты рецепторов подтипа 5-HT<sub>2B</sub> способны защищать сердце от вызываемой β-адренергическими агонистами, [[вазопрессин]]ом или [[ангиотензин II|ангиотензином II]] патологической гипертрофии сердечной мышцы у экспериментальных мышей.<ref name="pmid15302781">{{cite journal | author = Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L | title = Involvement of the serotonin 5-HT2B receptor in cardiac hypertrophy linked to sympathetic stimulation: control of interleukin-6, interleukin-1beta, and tumor necrosis factor-alpha cytokine production by ventricular fibroblasts | journal = Circulation | volume = 110 | issue = 8 | pages = 969–74 |date=August 2004 | pmid = 15302781 | doi = 10.1161/01.CIR.0000139856.20505.57 | url =  }}</ref><ref name="pmid18591460">{{cite journal | author = Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J | title = Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in mice | journal = Hypertension | volume = 52 | issue = 2 | pages = 301–7 |date=August 2008 | pmid = 18591460 | doi = 10.1161/HYPERTENSIONAHA.107.105551 | url =  }}</ref><ref name="pmid19023134">{{cite journal | author = Jaffré F, Bonnin P, Callebert J, Debbabi H, Setola V, Doly S, Monassier L, Mettauer B, Blaxall BC, Launay JM, Maroteaux L | title = Serotonin and Angiotensin Receptors in Cardiac Fibroblasts Coregulate Adrenergic-Dependent Cardiac Hypertrophy | journal = Circ. Res. | volume = 104| issue = 1| pages = 113–23|date=November 2008 | pmid = 19023134 | doi = 10.1161/CIRCRESAHA.108.180976 | url =  }}</ref>

* SERT: Рецепторы подтипа 5-HT<sub>2B</sub> регулируют методом обратной связи выделение [[серотонин]]а, влияя на активность белка-транспортера серотонина, и важны как для нормальной физиологической регуляции уровней серотонина в [[плазма крови|плазме]] [[кровь|крови]],<ref name="pmid16461587">{{cite journal | author = Callebert J, Esteve JM, Hervé P, Peoc'h K, Tournois C, Drouet L, Launay JM, Maroteaux L | title = Evidence for a control of plasma serotonin levels by 5-hydroxytryptamine(2B) receptors in mice | journal = J. Pharmacol. Exp. Ther. | volume = 317 | issue = 2 | pages = 724–31 |date=May 2006 | pmid = 16461587 | doi = 10.1124/jpet.105.098269 | url =  }}</ref> так и для ограничения аномального выброса серотонина, вызываемого такими веществами, как [[MDMA]].<ref name="pmid18337424">{{cite journal | author = Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L | title = Serotonin 5-HT2B 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 |date=March 2008 | pmid = 18337424 | doi = 10.1523/JNEUROSCI.5723-07.2008 | url =  }}</ref> Однако интересно, что активация рецепторов подтипа 5-HT<sub>2B</sub>, похоже, играет защитную роль против развития [[серотониновый синдром|серотонинового синдрома]], могущего возникнуть при резком повышении уровней внеклеточного серотонина,<ref name="pmid21277875">{{cite journal |author=Diaz SL, Maroteaux L |title=Implication of 5-HT(2B) receptors in the serotonin syndrome |journal=Neuropharmacology |volume= 61|issue= 3|pages= 495–502|date=January 2011 |pmid=21277875 |doi=10.1016/j.neuropharm.2011.01.025 |url=}}</ref> несмотря на его роль в модуляции высвобождения серотонина.

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== Клиническое значение ==

5-HT<sub>2B</sub> receptors have also been strongly implicated in drug-induced [[valvular heart disease]].<ref name="pmid11104741">{{cite journal | author = Rothman RB, Baumann MH, Savage JE, Rauser L, McBride A, Hufeisen SJ, Roth BL | title = Evidence for possible involvement of 5-HT(2B) receptors in the cardiac valvulopathy associated with fenfluramine and other serotonergic medications | journal = Circulation | volume = 102 | issue = 23 | pages = 2836–41 |date=December 2000 | pmid = 11104741 | doi =  10.1161/01.CIR.102.23.2836}}</ref><ref name="pmid10617681">{{cite journal | author = Fitzgerald LW, Burn TC, Brown BS, Patterson JP, Corjay MH, Valentine PA, Sun JH, Link JR, Abbaszade I, Hollis JM, Largent BL, Hartig PR, Hollis GF, Meunier PC, Robichaud AJ, Robertson DW | title = Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine | journal = Mol. Pharmacol. | volume = 57 | issue = 1 | pages = 75–81 |date=January 2000 | pmid = 10617681 | doi = }}</ref><ref name="pmid17202450">{{cite journal | author = Roth BL | title = Drugs and valvular heart disease | journal = N. Engl. J. Med. | volume = 356 | issue = 1 | pages = 6–9 |date=January 2007 | pmid = 17202450 | doi = 10.1056/NEJMp068265 }}</ref> In this context, it is generally considered to be an [[antitarget]].

The structure of the 5-HT<sub>2B</sub> receptor was recently solved in complex with the valvulopathogenic drug [[ergotamine]].<ref name="pmid23519215">{{PDB|4IB4}}; {{cite journal | author = Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC | title = Structural features for functional selectivity at serotonin receptors | journal = Science | volume = 340 | issue = 6132 | pages = 615–9 |date=May 2013 | pmid = 23519215 | doi = 10.1126/science.1232808 }}</ref>

== Лиганды ==

As of 2009, few highly selective 5-HT<sub>2B</sub> receptor ligands have been discovered, although numerous potent non-selective compounds are known, particularly agents with concomitant [[5-HT2C receptor|5-HT<sub>2C</sub>]] binding. Research in this area has been limited due to the cardiotoxicity of 5-HT<sub>2B</sub> agonists, and the lack of clear therapeutic application for 5-HT<sub>2B</sub> antagonists, but there is still a need for selective ligands for scientific research.<ref name="Schuhmacher">{{cite journal  | author = Schuhmacher M  | title = [Chiral arylmethoxytryptamines as 5-HT<sub>2B</sub>-receptor antagonists: synthesis, analysis and in-vitro pharmacology] (German)  | version = Ph.D. Dissertation | publisher =  University of Regensburg   | year = 2007 | pages = pages 6–17 | url = http://www.opus-bayern.de/uni-regensburg/volltexte/2008/796/pdf/Dissertation_Schumacher.pdf | accessdate = 2008-08-11 }}</ref>

=== Агонисты ===

==== Селективные ====
* [[BW-723C86]]:<ref name="pmid10498829">{{cite journal |author=Porter RH, Benwell KR, Lamb H, et al. |title=Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C 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=}}</ref> fair functional subtype selectivity; almost full agonist. Anxiolytic ''in vivo''.<ref name="pmid9886683">{{cite journal | author = Kennett GA, Trail B, Bright F | title = Anxiolytic-like actions of BW 723C86 in the rat Vogel conflict test are 5-HT2B receptor mediated | journal = Neuropharmacology | volume = 37 | issue = 12 | pages = 1603–10 |date=December 1998 | pmid = 9886683 | doi = 10.1016/S0028-3908(98)00115-4  | url =   }}</ref>
* [[Ro60-0175]]<ref name="pmid10498829"/> functionally selective over [[5-HT2A receptor|5-HT<sub>2A</sub>]], potent agonist at both 5-HT<sub>2B/C</sub>
* [[VER-3323]]: selective for 5-HT<sub>2B/C</sub> over 5-HT<sub>2A</sub>
* [[α-Methyl-5-HT]] — moderately selective over 5-HT<sub>2A/C</sub>
* [[6-APB]]

==== Неселективные ====

* [[MDMA]] (Ecstasy)<ref name="MDx">{{cite journal |author=Setola, Vincent |author2=Sandra J Hufeisen |author3=K Jane Grande-Allen |author4=Ivan Vesely |author5=Richard A Glennon |author6=Bruce Blough |author7=Richard B Rothman |author8=Bryan L Roth  |title=3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro |journal=Molecular Pharmacology |volume=63 |issue=6 |pages=1223&ndash;1229 | date= Jan 7, 2003 | doi=10.1124/mol.63.6.1223 |url=https://www.researchgate.net/publication/10748715_34-methylenedioxymethamphetamine_%28MDMA_Ecstasy%29_induces_fenfluramine-like_proliferative_actions_on_human_cardiac_valvular_interstitial_cells_in_vitro |pmid=12761331}}</ref>
* [[methylenedioxyamphetamine|MDA]]<ref name="MDx"/>
* [[2,5-Dimethoxy-4-ethoxyamphetamine|MEM]]<ref name="pmid20126400">{{cite journal | author = Ray TS | last2 = Manzoni | first2 = Olivier Jacques | title = Psychedelics and the Human Receptorome | journal = PLoS ONE | volume = 5 | issue = 2 | pages = e9019 | year = 2010 | pmid = 20126400 | pmc = 2814854 | doi = 10.1371/journal.pone.0009019 | url = | editor1-last = Manzoni | editor1-first = Olivier Jacques }}</ref>
* [[Pergolide]]<ref name="pmid18096760">{{cite 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<sub>2B</sub> and 5-Hydroxytryptamine<sub>2A</sub> receptors |journal=J. Pharmacol. Exp. Ther. |volume=324 |issue=3 |pages=1136–45 |year=2008 |pmid=18096760 |doi=10.1124/jpet.107.133165}}</ref>
* [[Cabergoline]]
* [[Norfenfluramine]]<ref name="pmid10498829"/>
* [[Chlorphentermine]]
* [[Aminorex]]
* [[1-(3-Chlorophenyl)piperazine|mCPP]]
* [[Bromo-dragonfly]]
* [[Dimethyltryptamine|DMT]]
* [[5-MeO-DMT]]

=== Антагонисты ===

* [[Sarpogrelate]]: a mixed 5-HT<sub>2A/B</sub> antagonist
* [[Lisuride]]: a [[dopamine agonist]] of the [[ergoline]] class, that is also a 5-HT<sub>2B</sub> antagonist<ref name="pmid16614540">{{cite journal | author = Hofmann C, Penner U, Dorow R, Pertz HH, Jähnichen S, Horowski R, Latté KP, Palla D, Schurad B | title = Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis | journal = Clin Neuropharmacol | volume = 29 | issue = 2 | pages = 80–6 | year = 2006 | pmid = 16614540 | doi = 10.1097/00002826-200603000-00005| url = http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?an=00002826-200603000-00005 }}</ref> and a dual 5-HT<sub>2A/C</sub> agonist<ref name="pmid9600588">{{cite journal |author=Egan CT, Herrick-Davis K, Miller K, Glennon RA, Teitler M |title=Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors |journal=Psychopharmacology (Berl.) |volume=136 |issue=4 |pages=409–14 |date=April 1998 |pmid=9600588 |doi=10.1007/s002130050585 |url=}}</ref>
* [[Tegaserod]]: primarily a 5-HT<sub>4</sub> agonist, but also a 5-HT<sub>2B</sub> antagonist<ref>{{cite journal |author=Beattie DT, Smith JA, Marquess D, et al. |title=The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo |journal=Br. J. Pharmacol. |volume=143 |issue=5 |pages=549–60 |date=November 2004 |pmid=15466450 |pmc=1575425 |doi=10.1038/sj.bjp.0705929 |url=}}</ref>
* [[RS-127,445]]:<ref name="pmid10455251">{{cite journal |author=Bonhaus DW, Flippin LA, Greenhouse RJ, et al. |title=RS-127445: a selective, high affinity, orally bioavailable 5-HT2B 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=}}</ref> high affinity; subtype selective (1000x), selective over at least eight other 5-HTR types; orally bioavailable.
* [[SDZ SER-082]]: a mixed 5-HT<sub>2B/C</sub> antagonist
* EGIS-7625: high selectivity over 5-HT<sub>2A</sub><ref name="pmid15107597">{{cite journal |author=Kovács A, Gacsályi I, Wellmann J, et al. |title=Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist |journal=Cardiovasc Drugs Ther |volume=17 |issue=5–6 |pages=427–34 |year=2003 |pmid=15107597 |doi= 10.1023/B:CARD.0000015857.96371.43|url=}}</ref>
* [[PRX-08066]]
* SB-200,646
* [[SB-204,741]]
* [[SB-206,553]]: mixed 5-HT<sub>2B/C</sub> antagonist and PAM at [[Alpha-7 nicotinic receptor#PAMs|α<sub>7</sub> nAChR]]<ref name="pmid19050173">{{cite journal |author=Dunlop J, Lock T, Jow B, et al. |title=Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide) |journal=J. Pharmacol. Exp. Ther. |volume=328 |issue=3 |pages=766–76 |date=March 2009 |pmid=19050173 |doi=10.1124/jpet.108.146514 |url=}}</ref>
* [[SB-215,505]]<ref name="pmid10188965">{{cite journal |author=Reavill C, Kettle A, Holland V, Riley G, Blackburn TP |title=Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist |journal=Br. J. Pharmacol. |volume=126 |issue=3 |pages=572–4 |date=February 1999 |pmid=10188965 |pmc=1565856 |doi=10.1038/sj.bjp.0702350 |url=}}</ref>
* SB-228,357
* [[LY-266,097]]
* [[LY-272,015]]

== Возможные клинические применения ==

5-HT<sub>2B</sub> antagonists have previously been proposed as treatment for [[migraine]] headaches, and RS-127,445 was trialled in humans up to Phase I for this indication, but development was not continued.<ref>{{cite journal |author=Poissonnet G, Parmentier JG, Boutin JA, Goldstein S |title=The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications |journal=Mini Rev Med Chem |volume=4 |issue=3 |pages=325–30 |date=March 2004 |pmid=15032678 |doi= 10.2174/1389557043487312|url=}}</ref> More recent research has focused on possible application of 5-HT<sub>2B</sub> antagonists as treatments for chronic [[heart disease]].<ref name="pmid19118279">{{cite journal |author=Shyu KG |title=Serotonin 5-HT2B receptor in cardiac fibroblast contributes to cardiac hypertrophy: a new therapeutic target for heart failure? |journal=Circulation Research |volume=104 |issue=1 |pages=1–3 |date=January 2009 |pmid=19118279 |doi=10.1161/CIRCRESAHA.108.191122 |url=}}</ref><ref name="pmid19307114">{{cite journal |author=Moss N, Choi Y, Cogan D, Flegg A, Kahrs A, Loke P, Meyn O, Nagaraja R, Napier S, Parker A, Thomas Peterson J, Ramsden P, Sarko C, Skow D, Tomlinson J, Tye H, Whitaker M |title=A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties |journal=Bioorganic & Medicinal Chemistry Letters |volume=19 |issue=8 |pages=2206–10 |date=April 2009 |pmid=19307114 |doi=10.1016/j.bmcl.2009.02.126 |url=}}</ref> Serotonin 5-HT2B receptors inhibit liver regeneration<ref name="pmid22120177">{{cite journal | author = Ebrahimkhani MR, Oakley F, Murphy LB, Mann J, Moles A, Perugorria MJ, Ellis E, Lakey AF, Burt AD, Douglass A, Wright MC, White SA, Jaffré F, Maroteaux L, Mann DA | title = Stimulating healthy tissue regeneration by targeting the 5-HT₂B receptor in chronic liver disease | journal = Nat. Med. | volume = 17 | issue = 12 | pages = 1668–73 |date=December 2011  | pmid = 22120177 | pmc = 3428919 | doi = 10.1038/nm.2490 }}</ref> and may have effects on immune system function.

--->

== См. также ==

* [[Серотониновые рецепторы]]

== Примечания ==

{{примечания|2}}

== Ссылки ==

* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2322 | title = 5-HT<sub>2B</sub>  | accessdate = | author = | authorlink = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}

== Для дополнительного чтения ==

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}}

[[Категория:Серотониновые рецепторы]]