5-HT1 receptor

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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 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:

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. 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
  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.{{cite journal}}: CS1 maint: article number as page number (link)
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