Department of Medical Pharmacology, Trakya University Faculty of Medicine, Edirne, Turkey.
Balkan Med J. 2014 Jun;31(2):115-20. doi: 10.5152/balkanmedj.2014.13103. Epub 2014 Jun 1.
Although cannabis has been used for pain management for millennia, very few approved cannabinoids are indicated for the treatment of pain and other medical symptoms. Cannabinoid therapy re-gained attention only after the discovery of endocannabinoids and fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), the enzymes playing a role in endocannabinoid metabolism. Nowadays, research has focused on the inhibition of these degradative enzymes and the elevation of endocannabinoid tonus locally; special emphasis is given on multi-target analgesia compounds, where one of the targets is the endocannabinoid degrading enzyme. In this review, I provide an overview of the current understanding about the processes accounting for the biosynthesis, transport and metabolism of endocannabinoids, and pharmacological approaches and potential therapeutic applications in this area, regarding the use of drugs elevating endocannabinoid levels in pain conditions.
尽管大麻已经被用于缓解疼痛数千年，但只有极少数经过批准的大麻素被用于治疗疼痛和其他医学症状。只有在发现内源性大麻素和脂肪酸酰胺水解酶（FAAH）和单酰基甘油脂肪酶（MAGL）后，大麻素治疗才重新受到关注，这两种酶在 内源性大麻素代谢中发挥作用。如今，研究的重点是抑制这些降解酶并局部提高内源性大麻素张力；特别强调多靶点镇痛化合物，其中一个靶点是内源性大麻素降解酶。在这篇综述中，我概述了当前对内源性大麻素生物合成、运输和代谢过程的理解，以及在这一领域使用药物来提高内源性大麻素水平治疗疼痛的药理学方法和潜在的治疗应用。
