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首页> 外文期刊>Current opinion in chemical biology >Fatty acid amide hydrolase: an emerging therapeutic target in the endocannabinoid system
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Fatty acid amide hydrolase: an emerging therapeutic target in the endocannabinoid system

机译:脂肪酸酰胺水解酶:内源性大麻素系统中的新兴治疗靶标

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The medicinal properties of exogenous cannabinoids have been recognized for centuries and can largely be attributed to the activation in the nervous system of a single G-protein-coupled receptor, CB1. However, the beneficial properties of cannabinoids, which include relief of pain and spasticity, are counterbalanced by adverse effects such as cognitive and motor dysfunction. The recent discoveries of anandamide, a natural lipid ligand for CB1, and an enzyme, fatty acid amide hydrolase (FAAH), that terminates anandamide signaling have inspired pharmacological strategies to augment endogenous cannabinoid ('endocannabinoid') activity with FAAH inhibitors, which might exhibit superior selectivity in their elicited behavioral effects compared with direct CB1 agonists.
机译:外源性大麻素的药用特性已有数百年历史,并且在很大程度上可归因于单个G蛋白偶联受体CB1在神经系统中的激活。但是,大麻素的有益特性(包括缓解疼痛和痉挛)被诸如认知和运动功能障碍之类的不利影响所抵消。最近发现的CB1天然脂质配体anandamide和终止anandamide信号传导的酶脂肪酸酰胺水解酶(FAAH)启发了药理学战略,希望通过FAAH抑制剂增强内源性大麻素('endocannabinoid')的活性。与直接的CB1激动剂相比,它们在引发的行为效果上具有更高的选择性。

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