Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA.
Bioorg Med Chem Lett. 2009 Oct 15;19(20):5931-5. doi: 10.1016/j.bmcl.2009.08.063. Epub 2009 Aug 21.
Replacement of the phenyl ring in our previous (morpholinomethyl)aniline carboxamide cannabinoid receptor ligands with a pyridine ring led to the discovery of a novel chemical series of CB2 ligands. Compound 3, that is, 2,2-dimethyl-N-(5-methyl-4-(morpholinomethyl)pyridin-2-yl)butanamide was identified as a potent and selective CB2 agonist exhibiting in vivo efficacy after oral administration in a rat model of neuropathic pain.
将我们之前的（吗啉甲基）苯胺甲酰胺大麻素受体配体中的苯基环替换为吡啶环，导致发现了一类新型的 CB2 配体。化合物 3，即 2,2-二甲基-N-(5-甲基-4-(吗啉甲基)吡啶-2-基)丁酰胺，被鉴定为一种有效的 CB2 激动剂，在神经病理性疼痛大鼠模型中经口服给药后具有体内疗效。
