3-Alkyl-(5,5'-diphenyl)imidazolidineiones as new cannabinoid receptor ligands.
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.
Kanyonyo
M
M
Unité de Chimie Pharmaceutique et de Radiopharmacie, Université Catholiqué de Louvain, Bruxelles, Belgium.
Govaerts
S J
SJ
Hermans
E
E
Poupaert
J H
JH
Lambert
D M
DM
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
D002186:Cannabinoids; D007093:Imidazoles; D008024:Ligands; D010880:Piperidines; D011720:Pyrazoles; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; D000077285:Rimonabant