大麻素受体2型
大麻素
大麻素受体
内大麻素系统
药物发现
药典
G蛋白偶联受体
医学
药理学
生物制药
计算生物学
神经科学
受体
生物信息学
生物
内科学
生物化学
病理
替代医学
兴奋剂
生药学
生物活性
体外
作者
Zak M. Whiting,Jiazhen Yin,Sara M. de la Harpe,Andrea J. Vernall,Natasha L. Grimsey
标识
DOI:10.1016/j.tips.2022.06.010
摘要
Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though as yet unrealised, therapeutic potential. Promising preclinical data supports the applicability of CB2 activation in autoimmune and inflammatory diseases, pain, neurodegeneration, and osteoporosis. A diverse pharmacopoeia of cannabinoid ligands is available, which has led to considerable advancements in the understanding of CB2 function and extensive preclinical evaluation. However, until recently, most CB2 ligands were highly lipophilic and as such not optimal for clinical application due to unfavourable physicochemical properties. A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties and a few such compounds have now undergone clinical trial. We review the current state of CB2 ligand development and progress in optimising physicochemical properties, understanding advanced molecular pharmacology such as functional selectivity, and clinical evaluation of CB2-targeting compounds.
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