Müller Christa E
Pharmazeutisches Institut, Pharmazeutische Chemie I, Universität Bonn, An der Immenburg 4, 53121, Bonn, Deutschland.
Pharma-Zentrum Bonn (PZB), Universität Bonn, Bonn, Deutschland.
Bundesgesundheitsblatt Gesundheitsforschung Gesundheitsschutz. 2019 Jul;62(7):818-824. doi: 10.1007/s00103-019-02964-4.
Preparations of hemp, Cannabis sativa, have been used for thousands of years as recreational and therapeutic drugs. The most important constituents are the psychoactive (-)-trans-∆-tetrahydrocannabinol (THC), a partial agonist at cannabinoid (CB) receptors CB and CB, and the non-psychoactive pleiotropic cannabidiol (CBD). Both compounds are highly lipophilic, like the endogenous CB receptor agonists, the arachidonic acid derivatives anandamide and arachidonoyl glycerol. The CB receptors belong to the family of G protein-coupled receptors, and the first X‑ray crystal structures of both CB receptors subtypes have recently been obtained, which will facilitate the rational design of novel synthetic ligands. Besides the already largely established indications such as chronic pain, chemotherapy-induced vomiting, multiple sclerosis-associated spasms, and cachexia, there is preliminary evidence for several further cannabinoid effects, which will have to be confirmed by clinical studies.
大麻(Cannabis sativa)制剂作为娱乐性和治疗性药物已被使用了数千年。其最重要的成分是具有精神活性的(-)-反式-Δ⁹-四氢大麻酚(THC),它是大麻素(CB)受体CB₁和CB₂的部分激动剂,以及无精神活性的多效性大麻二酚(CBD)。这两种化合物都具有高度的亲脂性,就像内源性CB受体激动剂、花生四烯酸衍生物花生四烯乙醇胺和花生四烯酰甘油一样。CB受体属于G蛋白偶联受体家族,最近已获得两种CB受体亚型的首个X射线晶体结构,这将有助于新型合成配体的合理设计。除了已经广泛确立的适应症,如慢性疼痛、化疗引起的呕吐、多发性硬化症相关的痉挛和恶病质外,还有一些关于大麻素其他作用的初步证据,这些证据有待临床研究证实。