Fowler Christopher J, Doherty Patrick, Alexander Stephen P H
Umeå University, Umeå, Sweden.
Wolfson Centre for Age-Related Disease, King's College London, London, United Kingdom.
Adv Pharmacol. 2017;80:31-66. doi: 10.1016/bs.apha.2017.03.006. Epub 2017 May 25.
In this review, we consider the biosynthetic, hydrolytic, and oxidative metabolism of the endocannabinoids anandamide and 2-arachidonoylglycerol. We describe the enzymes associated with these events and their characterization. We identify the inhibitor profile for these enzymes and the status of therapeutic exploitation, which to date has been limited to clinical trials for fatty acid amide hydrolase inhibitors. To bring the review to a close, we consider whether point block of a single enzyme is likely to be the most successful approach for therapeutic exploitation of the endocannabinoid system.
在本综述中,我们探讨了内源性大麻素花生四烯乙醇胺和2-花生四烯酸甘油酯的生物合成、水解及氧化代谢。我们描述了与这些过程相关的酶及其特性。我们确定了这些酶的抑制剂谱以及治疗开发的现状,迄今为止,这仅限于脂肪酸酰胺水解酶抑制剂的临床试验。为结束本综述,我们思考了对单一酶进行靶点阻断是否可能是治疗性开发内源性大麻素系统最成功的方法。