Chemistry:SB-228357

From HandWiki

SB-228357 is a drug which acts as a selective antagonist of the serotonin 5-HT2B and 5-HT2C receptors.[1][2]

It has antidepressant and anxiolytic effects in animal models[1][2] and inhibits 5-HT2B mediated proliferation of cardiac fibroblasts.[3] It has also been found to reverse meta-chlorophenylpiperazine (mCPP)-induced hypolocomotion[2] and to attenuate haloperidol-induced catalepsy.[1]

The drug was under development by GlaxoSmithKline for the treatment of major depressive disorder and anxiety disorders.[4] It reached the preclinical research phase of development.[4] However, development of the drug was discontinued.[4]

See also

References

  1. ↑ 1.0 1.1 1.2 "Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist". Br J Pharmacol 126 (3): 572–574. February 1999. doi:10.1038/sj.bjp.0702350. PMID 10188965. 
  2. ↑ 2.0 2.1 2.2 "Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent". Journal of Medicinal Chemistry 43 (6): 1123–34. March 2000. doi:10.1021/jm990388c. PMID 10737744. 
  3. ↑ "5-HT(2B) antagonism arrests non-canonical TGF-β1-induced valvular myofibroblast differentiation". Journal of Molecular and Cellular Cardiology 53 (5): 707–14. November 2012. doi:10.1016/j.yjmcc.2012.08.012. PMID 22940605. 
  4. ↑ 4.0 4.1 4.2 "SB 228357". 18 January 2008. https://adisinsight.springer.com/drugs/800013811. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:SB-228357&oldid=4175803"