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大麻素酸、类似物及内源性对应物。

The cannabinoid acids, analogs and endogenous counterparts.

作者信息

Burstein Sumner H

机构信息

Department of Biochemistry and Molecular Pharmacology, The University of Massachusetts Medical School, Worcester, MA 01605, USA.

出版信息

Bioorg Med Chem. 2014 May 15;22(10):2830-43. doi: 10.1016/j.bmc.2014.03.038. Epub 2014 Apr 1.

Abstract

The cannabinoid acids are a structurally heterogeneous group of compounds some of which are endogenous molecules and others that are metabolites of phytocannabinoids. The prototypic endogenous substance is N-arachidonoyl glycine (NAgly) that is closely related in structure to the cannabinoid agonist anandamide. The most studied phytocannabinoid is Δ(9)-THC-11-oic acid, the principal metabolite of Δ(9)-THC. Both types of acids have in common several biological actions such as low affinity for CB1 anti-inflammatory activity and analgesic properties. This suggests that there may be similarities in their mechanism of action, a point that is discussed in this review. Also presented are reports on analogs of the acids that provide opportunities for the development of novel therapeutic agents, such as ajulemic acid.

摘要

大麻素酸是一类结构异质的化合物,其中一些是内源性分子,另一些是植物大麻素的代谢产物。典型的内源性物质是N-花生四烯酰甘氨酸(NAgly),其结构与大麻素激动剂花生四烯乙醇胺密切相关。研究最多的植物大麻素是Δ(9)-四氢大麻酚-11-酸,它是Δ(9)-四氢大麻酚的主要代谢产物。这两类酸都具有多种生物学作用,如对CB1亲和力低、抗炎活性和镇痛特性。这表明它们的作用机制可能存在相似性,本综述将讨论这一点。还介绍了关于这些酸的类似物的报告,这些类似物为开发新型治疗药物提供了机会,如阿珠莫酸。

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