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A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity.

机译:一种新型单酰基甘油脂肪酶抑制剂,具有镇痛和抗炎活性。

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摘要

A variety of long chain 1,2-diamines and related compounds were synthesized and tested for their activity on fatty acid amide hydrolase (FAAH) and monoacyglycerol lipase (MGL). (2S,9Z)-Octadec-9-ene-1,2-diamine selectively inhibits MGL (K(i) 21.8 microM) without significantly affecting FAAH. This compound exhibited interesting in vivo analgesic and anti-inflammatory properties, suggesting that selective inhibitors of MGL may be valuable novel agents for the treatment of inflammatory pain.
机译:合成各种长链1,2-二胺和相关化合物,并在脂肪酸酰胺水解酶(FAAH)和单氰基甘油脂肪酶(MGL)上的活性测试。 (2S,9Z)-Octadec-9-Ene-1,2-二胺选择性地抑制MGL(K(I)21.8 microm),而不会显着影响FAAH。 该化合物表现出体内镇痛和抗炎性质的有趣,表明MGL的选择性抑制剂可能是治疗炎性疼痛的有价值的新药。

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