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).[1] The 5-HT1 subfamily consists of five G protein-coupled receptors (GPCRs) that share 40% to 63% overall sequence homology, including 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-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 to Gi/Go and mediate inhibitory neurotransmission by inhibiting the function of adenylate cyclase and modulating downstream ionic effects.[4] This R-coupling to Gi/Go proteins leads to a reduction in local concentrations of cAMP, proving that 5-HT1 are primarily inhibitory.[5] There is no 5-HT1C receptor, as it was reclassified as the 5-HT2C receptor.[6] 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

References
  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. 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, retrieved 2023-05-12
  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. Retrieved 26 Mar 2017.
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