5-HT receptor

In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT.cite journal | author = Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP | title = International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin) | journal = Pharmacol. Rev. | volume = 46 | issue = 2 | pages = 157–203 | year = 1994 | pmid = 7938165 | doi = | issn = | url = http://pharmrev.aspetjournals.org/cgi/content/abstract/46/2/157] cite book | author = Frazer A, Hensler JG | editor = Siegel GJ, Agranoff BW, Albers RW, Fisher SK, Uhler MD, editors | title = Basic Neurochemistry: Molecular, Cellular, and Medical Aspects | publisher = Lippincott-Raven | location = Philadelphia | year = 1999 | pages = | isbn = 0-397-51820-X | oclc = | doi = | pages = pages 263-292 | chapter= Chapter 13: Serotonin Receptors | chapterurl = http://www.ncbi.nlm.nih.gov/books/bv.fcgi?call=bv.View..ShowSection&rid=bnchm.section.963 | accessdate = 2008-04-11 ] 5-HT receptors are located on the cell membrane of nerve cells and other cell types including smooth muscle in animals, and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs. 5-HT receptors affect the release and activity of other neurotransmitters such as glutamate, dopamine and GABA. 5-HT_2A receptors increase the activity of glutamate in many areas of the brain, while some other serotonin receptors have the effect of suppressing glutamate. Increased stimulation of 5-HT_2A receptors seem to oppose the therapeutic actions of increased stimulation of other serotonin receptors in anti-depressant and anxiolytic treatments.cite journal | author = Marek GJ, Carpenter LL, McDougle CJ, Price LH | title = Synergistic action of 5-HT2A antagonists and selective serotonin reuptake inhibitors in neuropsychiatric disorders | journal = Neuropsychopharmacology | volume = 28 | issue = 2 | pages = 402–12 | year = 2003 | pmid = 12589395 | doi = 10.1038/sj.npp.1300057 ]

Classification

With the exception of the 5-HT₃ receptor, a ligand gated ion channel, all other 5-HT receptors are G protein coupled seven transmembrane (or "heptahelical") receptors that activate an intracellular second messenger cascade.

Families

pecific proteins/genes

Within these general classes of 5-HT receptors, a number of specific types have been characterized:cite web | url = http://www.acnp.org/g4/GN401000039/Ch039.html | title = Serotonin Receptor Subtypes and Ligands | accessdate = 2008-04-11 | author = Glennon RA, Dukat M, Westkaemper RB | authorlink = | coauthors = | date = 2000-01-01 | format = | work = | publisher = American College of Neurophyscopharmacology | pages = | language = | archiveurl = | archivedate = | quote = ] cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1288 | title = 5-Hydroxytryptamine Receptors | accessdate = 2008-04-11 | author = | authorlink = | coauthors = | date = | format = | work = IUPHAR Receptor Database | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = ] cite journal |author=Wesołowska A |title=In the search for selective ligands of 5-HT₅, 5-HT₆ and 5-HT₇ serotonin receptors |journal=Polish Journal of Pharmacology |volume=54 |issue=4 |pages=327–41 |year=2002 |pmid=12523486 |url=http://www.if-pan.krakow.pl/pjp/pdf/2002/4_327.pdf]

Note that there is no 5-HT_1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT₂ family of receptors and was redesignated as the 5-HT_2C receptor.

Therapeutic modulation

Various drugs are used to modulate the 5-HT system including some antidepressants, anxiolytics, antiemetics,antipsychotics and anti-migraine agents.cite journal | author = Nichols DE, Nichols CD | title = Serotonin receptors | journal = Chem. Rev. | volume = 108 | issue = 5 | pages = 1614–41 | year = 2008 | month = May | pmid = 18476671 | doi = 10.1021/cr078224o | url = | issn = ]

References

External links

*
*
*