Novel Benzimidazole Derivatives as Selective CB2 Inverse Agonists

D. Page; M.-C. Brochu; H. Yang; W. Brown; S. St-Onge; E. Martin; D. Salois

doi:10.2174/157018006777574177

ISSN: 1570-1808
E-ISSN: 1875-628X

Novel Benzimidazole Derivatives as Selective CB2 Inverse Agonists
Authors: D. Page¹, M.-C. Brochu², H. Yang³, W. Brown⁴, S. St-Onge⁵, E. Martin⁶ and D. Salois⁷
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¹ AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada. ² AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada. ³ AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada. ⁴ AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada. ⁵ AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada. ⁶ AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada. ⁷ AstraZeneca R&D Montreal, Department of Chemistry, 7171 Frederick-Banting, Ville St-Laurent, Quebec, H4S 1Z9, Canada.
Source: Letters in Drug Design & Discovery, Volume 3, Issue 5, Jul 2006, p. 298 - 303
DOI: https://doi.org/10.2174/157018006777574177
- Available online: 01 Jul 2006

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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2006-07-01

2025-09-08

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Article Type: Research Article

Keyword(s): benzimidazoles; Cannabinoids; CB2 receptor; inverse agonists

Novel Benzimidazole Derivatives as Selective CB2 Inverse Agonists

Abstract

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