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5-HT1 receptor

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Transmembrane protein
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This articleis missing information about some key characteristics that differentiate 5-HT1 as a whole from other 5-HT subtypes. Please expand the article to include this information. Further details may exist on thetalk page.(February 2017)


The5-HT1 receptors are a subfamily of the 5-HTserotonin receptors that bind to theendogenousneurotransmitterserotonin (also known as 5-hydroxytryptamine, or 5-HT).[1] 5-HT1 is not a standalone receptor. The 5-HT1 subfamily consists of fiveG protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including5-HT1A,5-HT1B,5-HT1D,5-HT1E, and5-HT1F.[2] Receptors of the 5-HT1 type, specifically, the 5-HT1A and 5-HT1D receptor subtypes, are present on the cell bodies. Receptors of the 5-HT1 type, specifically, the 5-HT1B and 5-HT1D 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.[3]

The receptor subfamily is coupled toGi/Go and mediatesinhibitoryneurotransmission by inhibiting the function of adenylate cyclase and modulating downstream ionic effects.[4] This R-coupling toGi/Go proteins leads to a reduction in local concentrations of cAMP, proving that 5-HT1 receptors are primarily inhibitory.[5] There is no 5-HT1C receptor, as it was reclassified as the5-HT2C receptor.[6]

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).[7] 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[8] 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 article:5-HT1A receptor
Main article:5-HT1B receptor
Main article:5-HT1D receptor
Main article:5-HT1E receptor
Main article:5-HT1F receptor

See also

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References

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  1. ^Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, Saxena PR, Humphrey PP (1994)."International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)".Pharmacol. Rev.46 (2):157–203.doi:10.1016/S0031-6997(25)06783-3.PMID 7938165.
  2. ^Hoyer, Daniel (2007-01-01), Enna, S. J.; Bylund, David B. (eds.),"5-HT-1 Receptors",xPharm: The Comprehensive Pharmacology Reference, New York: Elsevier, pp. 1–3,doi:10.1016/b978-008055232-3.60123-0,ISBN 978-0-08-055232-3, retrieved2023-05-12{{citation}}: CS1 maint: work parameter with ISBN (link)
  3. ^Bromidge, Steven M.; Bertani, Barbara; Borriello, Manuela; Bozzoli, Andrea; Faedo, Stefania; Gianotti, Massimo; Gordon, Laurie J.; Hill, Matthew; Zucchelli, Valeria; Watson, Jeannette M.; Zonzini, Laura (2009)."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".Bioorganic & Medicinal Chemistry Letters.19 (8):2338–2342.doi:10.1016/j.bmcl.2009.02.056.PMID 19286377.
  4. ^Lanfumey, Laurence; Hamon, Michel (2004)."5-HT1 Receptors".Current Drug Targets. CNS and Neurological Disorders.3 (1):1–10.doi:10.2174/1568007043482570.PMID 14965240.
  5. ^Comley, Robert A.; van der Aart, Jasper; Gulyás, Balázs; Garnier, Martine; Iavarone, Laura; Halldin, Christer; Rabiner, Eugenii A. (2015)."In vivo occupancy of the 5-HT1A receptor by a novel pan 5-HT1(A/B/D) receptor antagonist, GSK588045, using positron emission tomography".Neuropharmacology.92:44–48.doi:10.1016/j.neuropharm.2014.11.017.PMID 25476970.S2CID 144481206.
  6. ^"HTR2C 5-hydroxytryptamine receptor 2C [ Homo sapiens (human) ]".NCBI. 19 Mar 2017. Retrieved26 Mar 2017.
  7. ^Ślifirski, Grzegorz; Król, Marek; Turło, Jadwiga (2021-08-20)."5-HT Receptors and the Development of New Antidepressants".International Journal of Molecular Sciences.22 (16): 9015.doi:10.3390/ijms22169015.ISSN 1422-0067.PMC 8396477.PMID 34445721.
  8. ^Acharya, Ramesh; Sapkota, Sachin; Ruck, Lela; Abolbashari, Mehran (March 2025)."Sumatriptan-Induced Coronary Artery Vasospasm Leading to Acute ST Elevation Myocardial Infarction".Cureus.17 (3) e80920.doi:10.7759/cureus.80920.ISSN 2168-8184.PMC 12009358.PMID 40255801.
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5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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