Department of Pharmacy, University of Pisa, 56126 Pisa, Italy.
Pharmacol Res. 2021 Aug;170:105607. doi: 10.1016/j.phrs.2021.105607. Epub 2021 Jun 3.
In the last decades, cannabinoid receptor 2 (CBR) has continued to receive attention as a key therapeutic target in neuroprotection. Indeed, several findings highlight the neuroprotective effects of CBR through suppression of both neuronal excitability and reactive microglia. Additionally, CBR seems to be a more promising target than cannabinoid receptor 1 (CBR) thanks to the lack of central side effects, its lower expression levels in the central nervous system (CNS), and its inducibility, since its expression enhances quickly in the brain following pathological conditions. This review aims to provide a thorough overview of the main natural and synthetic selective CBR modulators, their chemical classification and their potential therapeutic usefulness in neuroprotection, a crucial aspect for the treatment of neurodegenerative diseases.
在过去的几十年中，大麻素受体 2 (CBR) 一直作为神经保护的关键治疗靶点受到关注。事实上，多项研究结果强调了 CBR 通过抑制神经元兴奋性和反应性小胶质细胞的双重作用发挥神经保护作用。此外，由于 CBR 在中枢神经系统 (CNS) 中的表达水平较低，缺乏中枢副作用，以及其可诱导性，即其表达在病理条件下可迅速增强，因此 CBR 似乎比大麻素受体 1 (CBR) 更有希望成为一个治疗靶点。本综述旨在全面概述主要的天然和合成选择性 CBR 调节剂、它们的化学分类以及它们在神经保护方面的潜在治疗用途，这是治疗神经退行性疾病的一个关键方面。
