Title: Novel Benzimidazole Derivatives as Selective CB2 Inverse Agonists
VOLUME: 3 ISSUE: 5
Author(s):D. Page, M.-C. Brochu, H. Yang, W. Brown, S. St-Onge, E. Martin and D. Salois
Affiliation:AstraZeneca R Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada.
Keywords:Cannabinoids, benzimidazoles, CB2 receptor, inverse agonists
Abstract: The preparation and evaluation of a novel class of CB2 benzimidazole inverse agonists are reported. They showed binding affinities up to 0.7 nM towards CB2 with overall good selectivity over the CB1 receptor. They also reversed the effect of the cannabinoid agonist WIN55212-2 in competition assays showing Ki values up to 1.2 nM.
