Biased Agonism at Cannabinoid CB1 and δ-Opioid Receptors; Therapeutic Potential

Cannabinoid CB1 (CB1R) and δ-opioid receptors (DOR) couple to a similar range of signal transduction systems and have similar physiological functions. Here we have characterised the signalling profiles of a number of standard and novel agonists at each of the receptors. Inhibition of forskolin-stimulated cyclic AMP accumulat ion, Erk42/44 MAP kinase phosphorylation and β2-arrestin recruitment were measured in CHO and HEK cells over-expressing human CB1R and DOR. Most CB1 agonists were biased (i.e.

Source: Neuropeptides - October 1, 2017 Category: Neuroscience Authors: David Kendall, Stephen Alexander, Richard Priestley, Muhammad Asghar, Bengt von Mentzer Source Type: research