SB-236057 explained
SB-236057 is a compound which is a potent and selective inverse agonist for the serotonin receptor 5-HT1B, acting especially at 5-HT1B autoreceptors on nerve terminals. It produces a rapid increase in serotonin levels in the brain, and was originally researched as a potential antidepressant.[1] [2] However subsequent research found that SB-236,057 also acts as a potent teratogen, producing severe musculoskeletal birth defects when rodents were exposed to it during pregnancy. This has made it of little use for research into its original applications, yet has made it useful for studying embryonic development instead.[3] [4]
Notes and References
- Middlemiss DN, Göthert M, Schlicker E, Scott CM, Selkirk JV, Watson J, Gaster LM, Wyman P, Riley G, Price GW . 6 . SB-236057, a selective 5-HT1B receptor inverse agonist, blocks the 5-HT human terminal autoreceptor . European Journal of Pharmacology . 375 . 1–3 . 359–65 . June 1999 . 10443589 . 10.1016/s0014-2999(99)00262-9 .
- Roberts C, Watson J, Price GW, Middlemiss DN . SB-236057-A: a selective 5-HT1B receptor inverse agonist . CNS Drug Reviews . 2006 . 7 . 4 . 433–44 . 10.1111/j.1527-3458.2001.tb00209.x . 11830759 . 6741665 .
- Augustine-Rauch KA, Zhang QJ, Posobiec L, Mirabile R, DeBoer LS, Solomon HM, Wier PJ . SB-236057: Critical window of sensitivity study and embryopathy of a potent musculoskeletal teratogen . Birth Defects Research. Part A, Clinical and Molecular Teratology . 70 . 10 . 773–88 . October 2004 . 15472921 . 10.1002/bdra.20079 .
- Augustine-Rauch KA, Zhang QJ, Leonard JL, Chadderton A, Welsh MJ, Rami HK, Thompson M, Gaster L, Wier PJ . 6 . Evidence for a molecular mechanism of teratogenicity of SB-236057, a 5-HT1B receptor inverse agonist that alters axial formation . Birth Defects Research. Part A, Clinical and Molecular Teratology . 70 . 10 . 789–807 . October 2004 . 15472891 . 10.1002/bdra.20076 .
