Mechoulam R, Fride E, Di Marzo V
Hebrew University, Medical Faculty, Jerusalem, Israel.
Eur J Pharmacol. 1998 Oct 16;359(1):1-18. doi: 10.1016/s0014-2999(98)00649-9.
The background knowledge leading to the isolation and identification of anandamide and 2-arachidonoyl glycerol, the principal endocannabinoids is described. The structure-activity relationships of these lipid derivatives are summarized. Selected biochemical and pharmacological topics in this field are discussed, the main ones being levels of endocannabinoids in unstimulated tissue and cells, biosynthesis, release and inactivation of endocannabinoids, the effects of 'entourage' compounds on the activities of anandamide and 2-arachidonoyl glycerol, their signaling mechanisms and effects in animals.
本文描述了导致分离和鉴定主要内源性大麻素——花生四烯乙醇胺和2-花生四烯酸甘油酯的背景知识。总结了这些脂质衍生物的构效关系。讨论了该领域中选定的生化和药理学主题,主要包括未受刺激的组织和细胞中的内源性大麻素水平、内源性大麻素的生物合成、释放和失活、“伴随”化合物对花生四烯乙醇胺和2-花生四烯酸甘油酯活性的影响、它们的信号传导机制以及在动物体内的作用。