The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats

Opioid agonists (e.g., oxycodone and morphine) are highly efficacious for the treatment of pain. However, their therapeutic effects are coupled with adverse side effects that include tolerance, dependence, respiratory depression, and abuse liability (Chan et al., 2017). Opioid agonists mediate their physiological actions through the G protein-coupled receptor (GPCR) family of opioid receptors, specifically the mu-opioid receptor (Kieffer, 1999; Matthes et al., 1996; Mello and Negus 1996). It is well established that GPCRs modify cell activity through various intracellular pathways including G-protein and b-arrestin signaling (Bologna et al., 2017), two pathways that are known to be prominent mediators of mu-opioid agonist effects (Bohn et al., 2004).
Source: Drug and Alcohol Dependence - Category: Addiction Authors: Tags: Full length article Source Type: research