Carfentanil is a β-arrestin-biased agonist at the μ opioid receptor.

ABSTRACT:

Background and purpose

The illicit use of fentanyl-like drugs (fentanyls), which are μ opioid receptor agonists, and the many overdose deaths that result, has become a major problem. Fentanyls are very potent in vivo, leading to respiratory depression and death. However, the efficacy and possible signalling bias of different fentanyls is not clearly known. Here, we compared the relative efficacy and bias of a series of fentanyls.

Experimental approach

For agonist signalling bias and efficacy measurements, Bioluminescence Resonance Energy Transfer experiments were undertaken in HEK293T cells transiently transfected with μ opioid receptors, to assess Gi protein activation and β-arrestin 2 recruitment. Agonist-induced cell surface receptor loss was assessed using an enzyme-link

SUBMITTER: Ramos-Gonzalez N 

PROVIDER: S-EPMC10952505 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature