Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.

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Plummer CW, Finke PE, Mills SG, Wang J, Tong X, Doss GA, Fong TM, Lao JZ, Schaeffer MT, Chen J, Shen CP, Stribling DS, Shearman LP, Strack AM, Van der Ploeg LH

Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6.

PubMed ID

15713403 [ View in PubMed

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Abstract

Structure-activity relationship studies directed toward the optimization of 4,5-diarylimidazole-2-carboxamide analogs as human CB1 receptor inverse agonists resulted in the discovery of the two amide derivatives 24a and b (hCB1 IC50 = 6.1 and 4.0 nM) which also demonstrated efficacy in overnight feeding studies in the rat for reduction in both food intake and overall body weight.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rimonabant	Cannabinoid receptor 1	IC 50 (nM)	6	N/A	N/A	Details