5-hydroxytryptamine receptor 2B
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[edit] Description
5-hydroxytryptamine (serotonin) receptor 2B, also known as HTR2B, is a 5-HT2 receptor, but also denotes the human gene encoding it.<ref name="entrez_ 3357">Template:Cite web</ref><ref name="pmid8143856">Schmuck K, Ullmer C, Engels P, Lübbert H (March 1994). "Cloning and functional characterization of the human 5-HT2B serotonin receptor". FEBS Lett. 342 (1): 85–90. PMID 8143856.</ref>
[edit] General Characterstics
[edit] Source Organism
Drosophila melanogaster (Fruit fly).
[edit] Taxomomy
Eukaryota; Metazoa; Arthropoda; Hexapoda; Insecta; Pterygota;Neoptera; Endopterygota; Diptera; Brachycera; Muscomorpha;Ephydroidea; Drosophilidae; Drosophila.
[edit] Subcellular Localization
Cell membrane; multi-pass membrane protein.
[edit] Similarity
Belongs to the G-protein coupled receptor 1 family.
[edit] Function
This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins which inhibit adenylate cyclase.The 5-HT2 receptors (of which the 5-HT2B 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.<ref name="entrez_ 3357"/>
The 5-HT2B receptor subtype is involved in:
- CNS: presynaptic inhibition, behavioural effects<ref name="pmid18337424">Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L (March 2008). "Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro". J. Neurosci. 28 (11): 2933–40. doi:. PMID 18337424.</ref>
- Vascular: pulmonary vasoconstriction<ref name="pmid12244304">Launay JM, Hervé P, Peoc'h K, Tournois C, Callebert J, Nebigil CG, Etienne N, Drouet L, Humbert M, Simonneau G, Maroteaux L (October 2002). "Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension". Nat. Med. 8 (10): 1129–35. doi:. PMID 12244304.</ref>
- Cardiac:The 5-HT2B receptor regulates cardiac structure and functions as demonstrated by the abnormal cardiac development observed in 5-HT2B receptor null mice.<ref name="pmid11413089">Nebigil CG, Hickel P, Messaddeq N, Vonesch JL, Douchet MP, Monassier L, György K, Matz R, Andriantsitohaina R, Manivet P, Launay JM, Maroteaux L (June 2001). "Ablation of serotonin 5-HT(2B) receptors in mice leads to abnormal cardiac structure and function". Circulation 103 (24): 2973–9. PMID 11413089.</ref> The 5-HT2B receptor stimulation can also lead to pathological proliferation of cardiac valves fibroblasts,<ref name="pmid18511249">Elangbam CS, Job LE, Zadrozny LM, Barton JC, Yoon LW, Gates LD, Slocum N (August 2008). "5-hydroxytryptamine (5HT)-induced valvulopathy: compositional valvular alterations are associated with 5HT2B receptor and 5HT transporter transcript changes in Sprague-Dawley rats". Exp. Toxicol. Pathol. 60 (4-5): 253–62. doi:. PMID 18511249.</ref> which with chronic overstimulation of 5-HT2B can lead to a severe valvulopathy. Moreover, 5-HT2B receptors were recently shown to be overexpressed in human failing heart and antagonists of 5-HT2B receptors were uncovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse.<ref name="pmid15302781">Jaffré F, Callebert J, Sarre A, Etienne N, Nebigil CG, Launay JM, Maroteaux L, Monassier L (August 2004). "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". Circulation 110 (8): 969–74. doi:. PMID 15302781.</ref><ref name="pmid18591460">Monassier L, Laplante MA, Jaffré F, Bousquet P, Maroteaux L, de Champlain J (August 2008). "Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in mice". Hypertension 52 (2): 301–7. doi:. PMID 18591460.</ref><ref name="pmid19023134">Jaffré F, Bonnin P, Callebert J, Debbabi H, Setola V, Doly S, Monassier L, Mettauer B, Blaxall BC, Launay JM, Maroteaux L (November 2008). "Serotonin and Angiotensin Receptors in Cardiac Fibroblasts Coregulate Adrenergic-Dependent Cardiac Hypertrophy". Circ. Res.. doi:. PMID 19023134.</ref>
- Serotonin transporter: 5-HT2B receptors regulate serotonin release via the serotonin transporter, and are important both to normal physiological regulation of serotonin levels in blood plasma,<ref name="pmid16461587">Callebert J, Esteve JM, Hervé P, Peoc'h K, Tournois C, Drouet L, Launay JM, Maroteaux L (May 2006). "Evidence for a control of plasma serotonin levels by 5-hydroxytryptamine(2B) receptors in mice". J. Pharmacol. Exp. Ther. 317 (2): 724–31. doi:. PMID 16461587.</ref> and with the abnormal acute serotonin release produced by drugs such as MDMA.<ref name="pmid18337424">Doly S, Valjent E, Setola V, Callebert J, Hervé D, Launay JM, Maroteaux L (March 2008). "Serotonin 5-HT2B receptors are required for 3,4-methylenedioxymethamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro". J. Neurosci. 28 (11): 2933–40. doi:. PMID 18337424.</ref>
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