I am a
Home I AM A Search Login

Papers of the Week

Papers: 30 Jul 2022 - 5 Aug 2022

Pharmacology/Drug Development

2022 Jul 26

Trends Pharmacol Sci

Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future.


Whiting ZM, Yin J, de la Harpe SM, Vernall AJ, Grimsey NL
Trends Pharmacol Sci. 2022 Jul 26.
PMID: 35906103.


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.