Mutation of putative GRK phosphorylation sites in the cannabinoid receptor 1 (CB1R) confers resistance to cannabinoid tolerance and hypersensitivity to cannabinoids in mice.
Journal of Neuroscience April 9, 2014 Daniel J Morgan, Brian J Davis, Chris S Kearn et al.
For many G-protein-coupled receptors (GPCRs), including cannabinoid receptor 1 (CB1R), desensitization has been proposed as a principal mechanism driving initial tolerance to agonists. GPCR desensitization typically requires phosphorylation by a G-protein-coupled receptor kinase (GRK) and interaction of the phosphorylated receptor with an arrestin. In simple model systems, CB1R is desensitized...
DOI: 10.1523/jneurosci.3445-12.2014 (opens in new tab)
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THC
Cb1
Gpcr
Cannabinoid
+2