期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 50, 期 11, 页码 2597-2600出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm061195+
关键词
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Selective CB2 receptor agonists are promising potential therapeutic agents for the treatment of inflammatory and neuropathic pain. A focused screen identified a pyrimidine ester as a partial agonist at the CB2 receptor with micromolar potency. Subsequent lead optimization identified 35, GW842166X, as the optimal compound in the series. 35 has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and was selected as a clinical candidate for this indication.
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