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A GPR18 antagonist
Selective GPR18 antagonist (IC50 = 0.279 μM). Exhibits >36-fold selectivity versus CB1 and GPR55 and 14-fold selectivity versus CB2 receptors. Inhibits N-Arachidonylglycine induced acrosomal exocytosis in human spermatozoa.
Rempel et al (2014) Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55. Med.Chem.Comm. 5 632 |Flegel et al (2016) Characterization of non-olfactory GPCRs in human sperm with a focus on GPR18. Sci.Rep. 6 32255 PMID:27572937
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