Novel Benzimidazole Derivatives as Selective CB2 Inverse Agonists

Author(s): D. Page , M.-C. Brochu , H. Yang , W. Brown , S. St-Onge , E. Martin , D. Salois .

Journal Name: Letters in Drug Design & Discovery

Volume 3 , Issue 5 , 2006

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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

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Article Details

VOLUME: 3
ISSUE: 5
Year: 2006
Page: [298 - 303]
Pages: 6
DOI: 10.2174/157018006777574177
Price: $58

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