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大麻素 1 型受体——药理学、在疼痛中的作用以及新型大麻素 1 型受体激动剂的最新进展。

Cannabinoid 1 (CB1) receptor--pharmacology, role in pain and recent developments in emerging CB1 agonists.

机构信息

Department of Preclinical Biology, Aurigene Discovery Technologies Ltd., Miyapur, Hyderabad, AP, India.

出版信息

CNS Neurol Disord Drug Targets. 2011 Aug;10(5):536-44. doi: 10.2174/187152711796235005.

DOI:10.2174/187152711796235005
PMID:21631407
Abstract

Cannabinoids are antinociceptive in animal models of acute pain, tissue injury and nerve injury induced nociception and act via their cognate receptors, cannabinoid receptor 1 and 2. This review examines the underlying biology of the endocannabinoids and behavioural, neurophysiological, neuroanatomical evidence supporting the notion of pain modulation by these ligands with a focus on the current evidence encompassing the pharmacological characterization of CB1 agonists in this therapy. Separating the psychotropic effects of CB1 agonists from their therapeutic benefits is the major challenge facing researchers in the field today and with the discovery of peripherally acting agonists there seems to be a ray of hope emerging for the diverse potential therapeutic applications of this class of ligands.

摘要

大麻素在急性疼痛、组织损伤和神经损伤引起的疼痛的动物模型中具有抗伤害作用,通过其同源受体大麻素受体 1 和 2 发挥作用。这篇综述检查了内源性大麻素的基础生物学,以及支持这些配体通过疼痛调制的行为、神经生理学、神经解剖学证据,重点是当前涵盖 CB1 激动剂在这种治疗中的药理学特征的证据。将 CB1 激动剂的精神作用与其治疗益处分开是该领域研究人员目前面临的主要挑战,随着外周作用激动剂的发现,这种配体的多种潜在治疗应用似乎出现了一线希望。

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