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
  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.