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三种植物大麻素:Δ⁹-四氢大麻酚、大麻二酚和Δ⁹-四氢大麻萜酚的不同CB1和CB2受体药理学特性

The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9-tetrahydrocannabinol, cannabidiol and delta9-tetrahydrocannabivarin.

作者信息

Pertwee R G

机构信息

School of Medical Sciences, Institute of Medical Sciences, University of Aberdeen, Aberdeen, UK.

出版信息

Br J Pharmacol. 2008 Jan;153(2):199-215. doi: 10.1038/sj.bjp.0707442. Epub 2007 Sep 10.

Abstract

Cannabis sativa is the source of a unique set of compounds known collectively as plant cannabinoids or phytocannabinoids. This review focuses on the manner with which three of these compounds, (-)-trans-delta9-tetrahydrocannabinol (delta9-THC), (-)-cannabidiol (CBD) and (-)-trans-delta9-tetrahydrocannabivarin (delta9-THCV), interact with cannabinoid CB1 and CB2 receptors. Delta9-THC, the main psychotropic constituent of cannabis, is a CB1 and CB2 receptor partial agonist and in line with classical pharmacology, the responses it elicits appear to be strongly influenced both by the expression level and signalling efficiency of cannabinoid receptors and by ongoing endogenous cannabinoid release. CBD displays unexpectedly high potency as an antagonist of CB1/CB2 receptor agonists in CB1- and CB2-expressing cells or tissues, the manner with which it interacts with CB2 receptors providing a possible explanation for its ability to inhibit evoked immune cell migration. Delta9-THCV behaves as a potent CB2 receptor partial agonist in vitro. In contrast, it antagonizes cannabinoid receptor agonists in CB1-expressing tissues. This it does with relatively high potency and in a manner that is both tissue and ligand dependent. Delta9-THCV also interacts with CB1 receptors when administered in vivo, behaving either as a CB1 antagonist or, at higher doses, as a CB1 receptor agonist. Brief mention is also made in this review, first of the production by delta9-THC of pharmacodynamic tolerance, second of current knowledge about the extent to which delta9-THC, CBD and delta9-THCV interact with pharmacological targets other than CB1 or CB2 receptors, and third of actual and potential therapeutic applications for each of these cannabinoids.

摘要

大麻是一组独特化合物的来源,这些化合物统称为植物大麻素或 phytocannabinoids。本综述聚焦于其中三种化合物,(-)-反式-δ9-四氢大麻酚(δ9-THC)、(-)-大麻二酚(CBD)和(-)-反式-δ9-四氢大麻萜酚(δ9-THCV)与大麻素 CB1 和 CB2 受体相互作用的方式。δ9-THC 是大麻的主要精神活性成分,是 CB1 和 CB2 受体的部分激动剂,与经典药理学一致,它引发的反应似乎受到大麻素受体的表达水平和信号传导效率以及内源性大麻素持续释放的强烈影响。在表达 CB1 和 CB2 的细胞或组织中,CBD 作为 CB1/CB2 受体激动剂的拮抗剂表现出出乎意料的高效能,其与 CB2 受体相互作用的方式为其抑制免疫细胞迁移的能力提供了一种可能的解释。δ9-THCV 在体外表现为强效的 CB2 受体部分激动剂。相比之下,它在表达 CB1 的组织中拮抗大麻素受体激动剂。它以相对较高的效能且以组织和配体依赖性方式做到这一点。当在体内给药时,δ9-THCV 也与 CB1 受体相互作用,表现为 CB1 拮抗剂,或在更高剂量下表现为 CB1 受体激动剂。本综述还简要提及了以下几点:一是 δ9-THC 产生的药效学耐受性,二是关于 δ9-THC、CBD 和 δ9-THCV 与 CB1 或 CB2 受体以外的药理学靶点相互作用程度的当前知识,三是这些大麻素各自的实际和潜在治疗应用。

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