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Review
. 2017 Feb:32:32-43.
doi: 10.1016/j.coph.2016.10.005. Epub 2016 Nov 9.

Cannabinoid receptor ligand bias: implications in the central nervous system

Robert B Laprairie  1 , Amina M Bagher  2 , Eileen M Denovan-Wright  3
Affiliations
Review

Cannabinoid receptor ligand bias: implications in the central nervous system

Robert B Laprairie et al. Curr Opin Pharmacol. 2017 Feb.

Abstract

The G protein-coupled cannabinoid receptors CB1, CB2, GPR18, and GPR55 regulate neurotransmission, pain, and inflammation and have been intensively investigated as potential drug _targets. Each of these GPCRs is coupled to multiple effector proteins mediating divergent cellular signals. The ligand bias of cannabinoid-_targeted compounds is only beginning to be quantified. Research into cannabinoid bias is now revealing correlations between bias in cell culture and functional outcomes in vivo. We present an example study of cannabinoid bias in the context of Huntington disease. In future, an understanding of cannabinoid receptor structure and quantification of ligand bias will optimize drug selection matched to patient population and disease.

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