Chemistry:SB-272183

From HandWiki

SB-272183 is a selective serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptor antagonist.[1][2][3] It shows high affinity for these receptors, with Ki values of 10 nM, 7.9 nM, and 2.0 nM, respectively, and with at least 30-fold selectivity over various other receptors.[1][2][4][3] The drug was a partial agonist of the serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptors in vitro, but showed only antagonistic activity ex vivo in native tissue.[1][2][3] SB-272183 was first described in the scientific literature in 2001.[3][5] It is said to have been the first selective serotonin 5-HT1A, 5-HT1B, and 5-HT1D receptor antagonist to be described.[2]

References

  1. ↑ 1.0 1.1 1.2 "Recent advances in 5-HT1B/1D receptor antagonists and agonists and their potential therapeutic applications". Current Topics in Medicinal Chemistry 2 (6): 559–574. June 2002. doi:10.2174/1568026023393903. PMID 12052194. 
  2. ↑ 2.0 2.1 2.2 2.3 "5-HT1 receptor augmentation strategies as enhanced efficacy: therapeutics for psychiatric disorders". Current Topics in Medicinal Chemistry 8 (12): 1008–1023. 2008. doi:10.2174/156802608785161439. PMID 18691129. 
  3. ↑ 3.0 3.1 3.2 3.3 "SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue". British Journal of Pharmacology 133 (6): 797–806. July 2001. doi:10.1038/sj.bjp.0704133. PMID 11454652. 
  4. ↑ "Ligands for the investigation of 5-HT autoreceptor function". Brain Research Bulletin 56 (5): 463–469. November 2001. doi:10.1016/s0361-9230(01)00628-1. PMID 11750791. 
  5. ↑ "Effects of 5-HT, fenfluramine, ketanserin and the 5-HT autoreceptor antagonist, SB-272183, on basal [H-3] 5-HT release from guinea-pig cortical slices in the presence and absence of paroxetine". British Journal of Pharmacology 134. November 2001. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:SB-272183&oldid=4583661"