PSB-SB-487
From Wikipedia, the free encyclopedia
 |
|
| Systematic (IUPAC) name | |
|---|---|
|
7-(1,1-Dimethyloctyl)-5-hydroxy-3-(2-hydroxybenzyl)-2H-chromen-2-one
|
|
| Identifiers | |
| PubChem | CID 70678101 |
| ChemSpider | 28667155 |
| Chemical data | |
| Formula | C26H32O4 |
| Molar mass | 408.53 |
|
|
|
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[edit]
References[edit]
- ^ 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
|
