Novel benzimidazole derivatives as selective CB2 agonists.

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Page D, Balaux E, Boisvert L, Liu Z, Milburn C, Tremblay M, Wei Z, Woo S, Luo X, Cheng YX, Yang H, Srivastava S, Zhou F, Brown W, Tomaszewski M, Walpole C, Hodzic L, St-Onge S, Godbout C, Salois D, Payza K

Novel benzimidazole derivatives as selective CB2 agonists.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3695-700. doi: 10.1016/j.bmcl.2008.05.073. Epub 2008 May 22.

PubMed ID

18522867 [ View in PubMed

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Abstract

The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dronabinol	Cannabinoid receptor 1	Ki (nM)	2.9	N/A	N/A	Details
Dronabinol	Cannabinoid receptor 2	Ki (nM)	41	N/A	N/A	Details
Dronabinol	Cannabinoid receptor 2	EC 50 (nM)	1.5	N/A	N/A	Details