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.
Keywords: Cannabinoids, benzimidazoles, CB2 receptor, inverse agonists
Letters in Drug Design & Discovery
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:
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.
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Cite this article as:
Page D., Brochu M.-C., Yang H., Brown W., St-Onge S., Martin E. and Salois D., Novel Benzimidazole Derivatives as Selective CB2 Inverse Agonists, Letters in Drug Design & Discovery 2006; 3 (5) . https://dx.doi.org/10.2174/157018006777574177
DOI https://dx.doi.org/10.2174/157018006777574177 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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