PSB-CB5 (1627710-30-8) is a potent and selective GPR18 antagonist (IC50?= 0.279 μM) exhibiting >36-fold selectivity against GPR55 and CB1 and 14-fold selectivity against CB2.1? Inhibits N-arachidonylglycine-induced acrosomal exocytosis in human spermatozoa indicating that GPR18 may be involved in physiological processes of human spermatozoa.2
1) 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
2) Flegel?et al.?(2016),?Characterization of Non-Olfactory GPCRs in Human Sperm With a Focus on GPR18; Sci. Rep.,?6?32255
