Br J Pharmacol. 2021 Jul 15. doi: 10.1111/bph.15627. Online ahead of print.


The cannabinoid receptor CB1 is the most abundant G protein coupled receptor (GPCR) in the central nervous system, which mediates the functional response to endocannabinoids and Cannabis compounds. A variety of ligands for CB1 have been developed as promising drug candidates for the treatment of neurological disorders. New high-resolution structures of CB1 in different functional states have significantly improved our molecular understanding of CB1 ligand interactions, selectivity, receptor activation and allosteric modulation. These advances have paved the way for development of novel ligands for different therapeutic applications. In this review, we describe the structural determinants for modulation of CB1 by different types of ligands, as well as the differences between CB1 and its homologous receptor CB2.

PMID:34265078 | DOI:10.1111/bph.15627

Source: ncbi 2

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