SB-236057

In this article we will address the topic of SB-236057, which has sparked great interest and debate in recent years. SB-236057 has aroused the curiosity of researchers, academics and the general public, due to its relevance in different areas of society. From its impact on the economy, politics, culture, to its influence on people's daily lives, SB-236057 has become a central topic of discussion and reflection. Along these lines we will analyze different perspectives and opinions about SB-236057, with the aim of offering a broad and enriching vision of this topic that is so relevant today.
SB-236057
Clinical data
ATC code
  • none
Identifiers
  • 1'-ethyl-5--2,3,6,7-tetrahydrospiro(furoindole-3,4'-piperidine)
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC33H34N4O3
Molar mass534.660 g·mol−1
3D model (JSmol)
  • n5nc(C)oc5-c(cc2C)ccc2-c6ccc(cc6)C(=O)N(CCc1cc3OC7)c1cc3C7(CC4)CCN4CC
  • InChI=1S/C33H34N4O3/c1-4-36-15-12-33(13-16-36)20-39-30-18-25-11-14-37(29(25)19-28(30)33)32(38)24-7-5-23(6-8-24)27-10-9-26(17-21(27)2)31-35-34-22(3)40-31/h5-10,17-19H,4,11-16,20H2,1-3H3
  • Key:WXAKEEQOWUHGCI-UHFFFAOYSA-N

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]

See also

References

  1. ^ Middlemiss DN, Göthert M, Schlicker E, Scott CM, Selkirk JV, Watson J, et al. (June 1999). "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. doi:10.1016/s0014-2999(99)00262-9. PMID 10443589.
  2. ^ Roberts C, Watson J, Price GW, Middlemiss DN (2006). "SB-236057-A: a selective 5-HT1B receptor inverse agonist". CNS Drug Reviews. 7 (4): 433–44. doi:10.1111/j.1527-3458.2001.tb00209.x. PMC 6741665. PMID 11830759.
  3. ^ Augustine-Rauch KA, Zhang QJ, Posobiec L, Mirabile R, DeBoer LS, Solomon HM, Wier PJ (October 2004). "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. doi:10.1002/bdra.20079. PMID 15472921.
  4. ^ Augustine-Rauch KA, Zhang QJ, Leonard JL, Chadderton A, Welsh MJ, Rami HK, et al. (October 2004). "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. doi:10.1002/bdra.20076. PMID 15472891.
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