Gómez-Ruiz María, Hernández Mariluz, de Miguel Rosario, Ramos Jose A
Departamento de Bioquímica y Biología Molecular III, Facultad de Medicina, Universidad Complutense, Ciudad Universitaria s/n, 28040 Madrid, Spain.
Mol Neurobiol. 2007 Aug;36(1):3-14. doi: 10.1007/s12035-007-0015-0. Epub 2007 Jun 30.
About 40 years ago, cannabinoids were considered as the substances responsible for the psychoactive properties of marijuana and other derivatives of Cannabis sativa, whereas their medicinal use remained unexplored. However, with the discovery of the endocannabinoid system 20 years later, the compounds able to modify this system are being reconsidered for their therapeutic potential. Thus, the term "cannabinoid" includes now much more compounds than those present in C. sativa derivatives, for instance, numerous synthetic cannabinoids obtained by modifications from plant-derived cannabinoids or from the compounds that behave as endogenous ligands for the different cannabinoid receptor types. The term "cannabinoid" should also refer to some prototypes of selective antagonists for these receptors. The explanation for this exponential growth in cannabinoid pharmacology is the discovery and characterization of the endocannabinoid signaling system (receptors, ligands, and inactivation system) which plays a modulatory role mainly in the brain but also in the periphery. The objective of the present review article was to give an overview of the present state-of-the-art of biochemistry of the endocannabinoid system. Other authors in this volume will review their functions in the brain, their alterations in a variety of neurological and psychiatric pathologies, and the proposed therapeutic benefits in these diseases of new cannabinoid-related compounds that improve the pharmacological properties of classic cannabinoids.
大约40年前,大麻素被认为是导致大麻及其他大麻属植物衍生物产生精神活性的物质,而它们的药用价值尚未得到探索。然而,20年后随着内源性大麻素系统的发现,能够调节该系统的化合物因其治疗潜力而被重新审视。因此,“大麻素”一词现在所涵盖的化合物比大麻属植物衍生物中的化合物要多得多,例如,许多通过对植物源性大麻素或作为不同类型大麻素受体的内源性配体的化合物进行修饰而获得的合成大麻素。“大麻素”一词还应指代这些受体的一些选择性拮抗剂原型。大麻素药理学呈指数级增长的原因在于内源性大麻素信号系统(受体、配体和失活系统)的发现和表征,该系统主要在大脑中发挥调节作用,也在外周发挥作用。本综述文章的目的是概述内源性大麻素系统生物化学的当前研究现状。本卷中的其他作者将综述它们在大脑中的功能、在各种神经和精神疾病中的改变,以及新的大麻素相关化合物在这些疾病中的潜在治疗益处,这些新化合物改善了经典大麻素的药理特性。