PSB-SB-487
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This is an old revision of this page, as edited by Ffffrr (talk | contribs) at 03:51, 13 April 2022 (Importing Wikidata short description: "Chemical compound" (Shortdesc helper)). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.
Revision as of 03:51, 13 April 2022 by Ffffrr (talk | contribs) (Importing Wikidata short description: "Chemical compound" (Shortdesc helper))
Chemical compound
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Formula | C26H32O4 |
Molar mass | 408.53 g·mol−1 |
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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 CE (June 2013). "Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold". Journal of Medicinal Chemistry. 56 (11): 4798–810. doi:10.1021/jm4005175. PMID 23679955.
- ^ Rempel V, Volz N, Hinz S, Karcz T, Meliciani I, Nieger M, et al. (September 2012). "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. doi:10.1021/jm3008213. PMID 22916707.
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