Biochemistry and pharmacology of the endocannabinoids arachidonylethanolamide and 2-arachidonylglycerol

被引：203

作者：

Hillard, CJ ^{[1
]}

机构：

[1] Med Coll Wisconsin, Dept Pharmacol & Toxicol, Milwaukee, WI 53226 USA

来源：

PROSTAGLANDINS & OTHER LIPID MEDIATORS | 2000年 / 61卷 / 1-2期

关键词：

cannabinoids; anandamide; N-arachidonylphosphatidylethanolamine; fatty acid amide hydrolase; CB1; receptor; reproduction; gastrointestinal;

D O I：

10.1016/S0090-6980(00)00051-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The purpose of this review is to discuss the cellular synthesis and inactivation of two putative endogenous ligands of the cannabinoid receptor, N-arachidonylethanolamine (AEA) and 2-arachidonylglycerol (2-AG). Both ligands are synthesized by neurons and brain tissue in response to increased intracellular calcium concentrations. Both ligands are substrates for fatty acid amide hydrolase (FAAH). Both AEA and 2-AG bind to the neuronal form of the cannabinoid receptor (CBI). AEA binds the receptor with moderate affinity and has the characteristics of a partial agonist, whereas, 2-AG binds with low affinity but exhibits full efficacy. Two possible physiological roles of the endocannabinoids and the CB1 receptor are discussed: the regulation of gestation and the regulation of gastrointestinal motility. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：3 / 18

页数：16

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