Chromenopyrazole-based High Affinity, Selective Fluorescent Ligands for Cannabinoid Type 2 Receptor.

ABSTRACT: Cannabinoid type 2 receptor (CB₂R) is an attractive target for the treatment of pain and inflammatory disorders. Availability of a selective CB₂R fluorescent ligand to study CB₂R expression and localization in healthy and disease conditions would greatly contribute to improving our understanding of this receptor. Herein, we report a series of chromenopyrazole-based CB₂R fluorescent ligands. The highest affinity fluorescent ligand was Cy5-containing 24 (hCB₂R pK _i = 7.38 ± 0.05), which had 131-fold selectivity over CB₁R. In a cAMP BRET assay, 24 behaved as a potent CB₂R inverse agonist. Widefield imaging experiments showed that 24 binds to CB₂R in live cells with go

SUBMITTER: Singh S 

PROVIDER: S-EPMC6378661 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature