Article · Wikipedia archive · Last revised Jul 25, 2026

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). 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-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. 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.

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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 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-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 mediates 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 receptors are primarily inhibitory.5 There is no 5-HT1C receptor, as it was reclassified as the 5-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 pain8 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:

See also

See also

References

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. 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, retrieved 2023-05-12{{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. Retrieved 26 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.