5-HT1 receptor

{{Short description|Transmembrane protein}} {{context|date=February 2017}} {{missing information | some key characteristics that differentiate 5-HT₁ as a whole from other 5-HT subtypes|date=February 2017}}

{{DISPLAYTITLE:5-HT₁ receptor}}

The '''5-HT₁ receptors''' are a subfamily of the 5-HT serotonin receptors that bind to the endogenous neurotransmitter serotonin (also known as 5-hydroxytryptamine, or 5-HT).<ref name="pmid7938165">{{cite journal | vauthors = 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 | doi = 10.1016/S0031-6997(25)06783-3 | pmid = 7938165 | url = http://pharmrev.aspetjournals.org/cgi/content/abstract/46/2/157| url-access = subscription }}</ref> 5-HT₁ is not a standalone receptor. The 5-HT₁ subfamily consists of five G protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_1E, and 5-HT_1F.<ref>{{Citation |last=Hoyer |first=Daniel |title=5-HT-1 Receptors |date=2007-01-01 |url=https://www.sciencedirect.com/science/article/pii/B9780080552323601230 |work=xPharm: The Comprehensive Pharmacology Reference |pages=1–3 |editor-last=Enna |editor-first=S. J. |access-date=2023-05-12 |place=New York |publisher=Elsevier |language=en |doi=10.1016/b978-008055232-3.60123-0 |isbn=978-0-08-055232-3 |editor2-last=Bylund |editor2-first=David B.|url-access=subscription }}</ref> Receptors of the 5-HT₁ type, specifically, the 5-HT_1A and 5-HT_1D receptor subtypes, are present on the cell bodies. Receptors of the 5-HT1 type, specifically, the 5-HT_1B and 5-HT_1D receptor subtypes, are also present on the nerve terminals. These receptors are broadly distributed throughout the brain and are recognized to play a significant part in regulating synaptic levels of 5-HT.<ref>{{Cite journal |last1=Bromidge |first1=Steven M. |last2=Bertani |first2=Barbara |last3=Borriello |first3=Manuela |last4=Bozzoli |first4=Andrea |last5=Faedo |first5=Stefania |last6=Gianotti |first6=Massimo |last7=Gordon |first7=Laurie J. |last8=Hill |first8=Matthew |last9=Zucchelli |first9=Valeria |last10=Watson |first10=Jeannette M. |last11=Zonzini |first11=Laura |title=8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors—Part II |url=https://linkinghub.elsevier.com/retrieve/pii/S0960894X09002108 |journal=Bioorganic & Medicinal Chemistry Letters |year=2009 |language=en |volume=19 |issue=8 |pages=2338–2342 |doi=10.1016/j.bmcl.2009.02.056|pmid=19286377 |url-access=subscription }}</ref>

The receptor subfamily is coupled to G_i/G_o and mediates inhibitory neurotransmission by inhibiting the function of adenylate cyclase and modulating downstream ionic effects.<ref>{{Cite journal |last1=Lanfumey |first1=Laurence |last2=Hamon |first2=Michel |title=5-HT1 Receptors |url=https://www.eurekaselect.com/article/36093 |journal=Current Drug Targets. CNS and Neurological Disorders |year=2004 |language=en |volume=3 |issue=1 |pages=1–10 |doi=10.2174/1568007043482570|pmid=14965240 |url-access=subscription }}</ref> This R-coupling to G_i/G_o proteins leads to a reduction in local concentrations of cAMP, proving that 5-HT₁ receptors are primarily inhibitory.<ref>{{Cite journal |last1=Comley |first1=Robert A. |last2=van der Aart |first2=Jasper |last3=Gulyás |first3=Balázs |last4=Garnier |first4=Martine |last5=Iavarone |first5=Laura |last6=Halldin |first6=Christer |last7=Rabiner |first7=Eugenii A. |title=In vivo occupancy of the 5-HT1A receptor by a novel pan 5-HT1(A/B/D) receptor antagonist, GSK588045, using positron emission tomography |url=https://linkinghub.elsevier.com/retrieve/pii/S002839081400433X |journal=Neuropharmacology |year=2015 |language=en |volume=92 |pages=44–48 |doi=10.1016/j.neuropharm.2014.11.017|pmid=25476970 |s2cid=144481206 |url-access=subscription }}</ref> There is no 5-HT_1C receptor, as it was reclassified as the 5-HT_2C receptor.<ref>{{cite web |url= https://www.ncbi.nlm.nih.gov/gene?cmd=Retrieve&dopt=full_report&list_uids=3358 |title= HTR2C 5-hydroxytryptamine receptor 2C [ Homo sapiens (human) ] |date= 19 Mar 2017 |website= NCBI |access-date= 26 Mar 2017}}</ref>

5-HT₁ is one of seven families that make up the complete subtypes of 5-HT serotonin receptors. It is represented by the number 1, and the five subtypes are represented by letters (e.g., a, b, c, d).<ref>{{Cite journal |last1=Ślifirski |first1=Grzegorz |last2=Król |first2=Marek |last3=Turło |first3=Jadwiga |date=2021-08-20 |title=5-HT Receptors and the Development of New Antidepressants |journal=International Journal of Molecular Sciences |language=en |volume=22 |issue=16 |page=9015 |doi=10.3390/ijms22169015 |doi-access=free |issn=1422-0067 |pmc=8396477 |pmid=34445721}}</ref> Unlike other 5-HT subtype receptors, several 5-HT₁ subtypes play a role in pain relief from migraine headaches. The interaction between Serotonin agonists, like Triptans, and these subtypes helps relieve migraine pain<ref>{{Cite journal |last1=Acharya |first1=Ramesh |last2=Sapkota |first2=Sachin |last3=Ruck |first3=Lela |last4=Abolbashari |first4=Mehran |date=March 2025 |title=Sumatriptan-Induced Coronary Artery Vasospasm Leading to Acute ST Elevation Myocardial Infarction |journal=Cureus |volume=17 |issue=3 |article-number=e80920 |doi=10.7759/cureus.80920 |doi-access=free |issn=2168-8184 |pmc=12009358 |pmid=40255801 }}</ref> There has been and continues to be extensive research on 5-HT₁ and anti-migraine drugs.

For more information, please see the respective main articles of the individual subtypes:

{{Main|5-HT1A receptor}} {{Main|5-HT1B receptor}}

{{Main|5-HT1D receptor}}

{{Main|5-HT1E receptor}}

{{Main|5-HT1F receptor}}

==See also== * 5-HT₂ receptor * 5-HT₃ receptor * 5-HT₄ receptor * 5-HT₅ receptor * 5-HT₆ receptor * 5-HT₇ receptor

==References== {{reflist}}

{{G protein-coupled receptors}} {{Cell signaling}} {{Serotonergics}}

Category:Serotonin receptors

{{biochem-stub}}