Chemistry:SB-224289

From HandWiki

SB-224289 is a selective serotonin 5-HT1B receptor antagonist or inverse agonist which is used in scientific research.[1][2][3][4][5] It is more than 75-fold selective for the serotonin 5-HT1B receptor over all other serotonin receptors.[3] The drug indirectly increases serotonin release by blocking inhibitory serotonin 5-HT1B autoreceptors.[1][3] In addition to its serotonin 5-HT1B receptor antagonism, SB-224289 has subsequently been found to counteract the antifungal effects of the marine depsipeptide papuamide A.[6]

References

  1. ↑ 1.0 1.1 "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. 
  2. ↑ "Failure to detect in vivo inverse agonism of the 5-HT(1B) receptor antagonist SB-224289 in 5-HT-depleted guinea-pigs". Naunyn-Schmiedeberg's Archives of Pharmacology 365 (6): 462–467. June 2002. doi:10.1007/s00210-002-0564-8. PMID 12070760. 
  3. ↑ 3.0 3.1 3.2 "SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity". British Journal of Pharmacology 125 (1): 202–208. September 1998. doi:10.1038/sj.bjp.0702059. PMID 9776361. 
  4. ↑ "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. 
  5. ↑ "The selective 5-HT1B receptor inverse agonist (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo". Journal of Medicinal Chemistry 41 (8): 1218–1235. April 1998. doi:10.1021/jm970457s. PMID 9548813. 
  6. ↑ "SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A". PLOS ONE 11 (5). 2016. doi:10.1371/journal.pone.0154932. PMID 27183222. Bibcode: 2016PLoSO..1154932C. 



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