title: 3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.
abstract: Twenty-four 3-alkyl-(5,5'-diphenyl)imidazolidinediones were synthesized and evaluated as new cannabinoid receptor ligands. Three compounds exhibited a Ki value around 100 nM against [3H]-SR 141716A binding obtained from human CB1 transfected CHO cells membranes. The lack of change of affinity in the presence of a non hydrolyzable GTP analogue seems to indicate they are cannabinoid antagonists.
authors.affiliation: Unité de Chimie Pharmaceutique et de Radiopharmacie, Université Catholiqué de Louvain, Bruxelles, Belgium.
authors.forename: M
authors.initials: M
authors.lastname: Kanyonyo
authors.forename: S J
authors.initials: SJ
authors.lastname: Govaerts
authors.forename: E
authors.initials: E
authors.lastname: Hermans
authors.forename: J H
authors.initials: JH
authors.lastname: Poupaert
authors.forename: D M
authors.initials: DM
authors.lastname: Lambert
mesh_terms: D000818:Animals; D016466:CHO Cells; D002186:Cannabinoids; D006224:Cricetinae; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008024:Ligands; D010880:Piperidines / Q000494:pharmacology; D011720:Pyrazoles / Q000494:pharmacology; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000037:antagonists & inhibitors*; D000077285:Rimonabant; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D002186:Cannabinoids; D007093:Imidazoles; D008024:Ligands; D010880:Piperidines; D011720:Pyrazoles; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; D000077285:Rimonabant