Chemistry:PSB-SB-487
From HandWiki
Short description: Chemical compound
 | |
| Identifiers | |
|---|---|
| |
| PubChem CID | |
| ChemSpider | |
| Chemical and physical data | |
| Formula | C26H32O4 |
| Molar mass | 408.53 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
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
- ↑ "Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold". Journal of Medicinal Chemistry 56 (11): 4798–810. June 2013. doi:10.1021/jm4005175. PMID 23679955. https://figshare.com/articles/journal_contribution/2405257.
- ↑ "7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists". Journal of Medicinal Chemistry 55 (18): 7967–77. September 2012. doi:10.1021/jm3008213. PMID 22916707.
 |  |
