5-hydroxytryptamine receptor 2B
From DrugPedia: A Wikipedia for Drug discovery
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| - | + | ==Description== | |
| - | ==Source Organism== | + | '''5-hydroxytryptamine (serotonin) receptor 2B''', also known as '''HTR2B''', is a [[5-HT2 receptor|5-HT<sub>2</sub> receptor]], but also denotes the human [[gene]] encoding it.<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 | year = 1994 | month = March | pmid = 8143856 | doi = | url = http://linkinghub.elsevier.com/retrieve/pii/0014-5793(94)80590-3 | issn = }}</ref> |
| + | ==General Characterstics== | ||
| + | ===Source Organism=== | ||
Drosophila melanogaster (Fruit fly). | Drosophila melanogaster (Fruit fly). | ||
| - | ==Taxomomy== | + | ===Taxomomy=== |
Eukaryota; Metazoa; Arthropoda; Hexapoda; Insecta; Pterygota;Neoptera; Endopterygota; Diptera; Brachycera; Muscomorpha;Ephydroidea; Drosophilidae; Drosophila. | Eukaryota; Metazoa; Arthropoda; Hexapoda; Insecta; Pterygota;Neoptera; Endopterygota; Diptera; Brachycera; Muscomorpha;Ephydroidea; Drosophilidae; Drosophila. | ||
| - | ==Subcellular Localization== | + | ===Subcellular Localization=== |
Cell membrane; multi-pass membrane protein. | Cell membrane; multi-pass membrane protein. | ||
| - | |||
| - | ==Similarity== | + | ===Similarity=== |
Belongs to the G-protein coupled receptor 1 family. | Belongs to the G-protein coupled receptor 1 family. | ||
| - | |||
==Function== | ==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. | + | 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-HT<sub>2</sub> receptors (of which the 5-HT<sub>2B</sub> 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 [[amphetamine|phenylisopropylamine]] [[hallucinogen]]s.<ref name="entrez_ 3357"/> |
| + | |||
| + | The 5-HT<sub>2B</sub> receptor subtype is involved in: | ||
| + | * CNS: [[presynaptic inhibition]], behavioural effects<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 | year = 2008 | month = March | pmid = 18337424 | doi = 10.1523/JNEUROSCI.5723-07.2008 | url = | issn = }}</ref> | ||
| + | * Vascular: pulmonary [[vasoconstriction]]<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 | year = 2002 | month = October | pmid = 12244304 | doi = 10.1038/nm764 | url = | issn = }}</ref> | ||
| + | * Cardiac:The 5-HT<sub>2B</sub> receptor regulates cardiac structure and functions as demonstrated by the abnormal cardiac development observed in 5-HT<sub>2B</sub> receptor null mice.<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 | year = 2001 | month = June | pmid = 11413089 | doi = | url = http://circ.ahajournals.org/cgi/content/abstract/103/24/2973 | issn = }}</ref> The 5-HT<sub>2B</sub> receptor stimulation can also lead to pathological proliferation of cardiac valves fibroblasts,<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 | year = 2008 | month = August | pmid = 18511249 | doi = 10.1016/j.etp.2008.03.005 | url = | issn = }}</ref> which with chronic overstimulation of 5-HT<sub>2B</sub> can lead to a severe valvulopathy. Moreover, 5-HT<sub>2B</sub> receptors were recently shown to be overexpressed in human failing heart and antagonists of 5-HT<sub>2B</sub> receptors were uncovered to prevent both angiotensin II or beta-adrenergic agonist-induced pathological cardiac hypertrophy in mouse.<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 | year = 2004 | month = August | pmid = 15302781 | doi = 10.1161/01.CIR.0000139856.20505.57 | url = | issn = }}</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 | year = 2008 | month = August | pmid = 18591460 | doi = 10.1161/HYPERTENSIONAHA.107.105551 | url = | issn = }}</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 = | issue = | pages = | year = 2008 | month = November | pmid = 19023134 | doi = 10.1161/CIRCRESAHA.108.180976 | url = | issn = }}</ref> | ||
| + | |||
| + | * [[Serotonin transporter]]: 5-HT<sub>2B</sub> 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">{{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 | year = 2006 | month = May | pmid = 16461587 | doi = 10.1124/jpet.105.098269 | url = | issn = }}</ref> and with the abnormal acute serotonin release produced by drugs such as [[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 | year = 2008 | month = March | pmid = 18337424 | doi = 10.1523/JNEUROSCI.5723-07.2008 | url = | issn = }}</ref> | ||
[[Categories:Receptors]] | [[Categories:Receptors]] | ||
| + | {{Wrongtitle|title=5-HT<sub>2B</sub> receptor}} | ||
| + | {{PBB|geneid=3357}} | ||
| + | |||
| + | |||
| + | ==External links== | ||
| + | * {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2322 | title = 5-HT<sub>2B</sub> | accessdate = | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }} | ||
| + | |||
| + | ==References== | ||
Revision as of 11:28, 16 February 2009
Contents |
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>
General Characterstics
Source Organism
Drosophila melanogaster (Fruit fly).
Taxomomy
Eukaryota; Metazoa; Arthropoda; Hexapoda; Insecta; Pterygota;Neoptera; Endopterygota; Diptera; Brachycera; Muscomorpha;Ephydroidea; Drosophilidae; Drosophila.
Subcellular Localization
Cell membrane; multi-pass membrane protein.
Similarity
Belongs to the G-protein coupled receptor 1 family.
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>
Categories:Receptors Template:Wrongtitle Template:PBB
