PSB-SB-487
 | |
| Identifiers | |
|---|---|
| |
| PubChem (CID) | 70678101 |
| ChemSpider | 28667155 |
| Chemical and physical data | |
| Formula | C26H32O4 |
| Molar mass | 408.53 |
| 3D model (Jmol) | Interactive image |
| |
| |
PSB-SB-487 is a coumarin derivative which is an antagonist at the former orphan receptor GPR55. Unlike older GPR55 antagonists such as O-1918, PSB-SB-487 has good selectivity over the related receptor GPR18, with an IC50 of 113nM at GPR55 vs 12500nM at GPR18.[1] However it has poorer selectivity over other related receptors, acting as a weak antagonist at CB1 with a Ki of 1170nM, and a partial agonist at CB2 with a Ki of 292nM.[2]
See also
References
- ↑ Rempel, V.; Volz, N.; Gläser, F.; Nieger, M.; Bräse, S.; Müller, C. E. (2013). "Antagonists for the orphan G protein-coupled receptor GPR55 based on a coumarin scaffold". Journal of Medicinal Chemistry. 56 (11): 130516144836005. doi:10.1021/jm4005175. PMID 23679955.
- ↑ Rempel V, Volz N, Hinz S, Karcz T, Meliciani I, Nieger M, Wenzel W, Bräse S, Müller CE. 7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists. Journal of Medicinal Chemistry. 2012 Sep 27;55(18):7967-77. PMID 22916707
This article is issued from Wikipedia - version of the 4/2/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.