A6V polymorphism of the human μ-opioid receptor decreases signalling of morphine and endogenous opioids in vitro.

ABSTRACT:

Background and purpose

Polymorphisms of the μ opioid receptor (MOPr) may contribute to the variation in responses to opioid drugs in clinical and unregulated situations. The A6V variant of MOPr (MOPr-A6V) is present in up to 20% of individuals in some populations, and may be associated with heightened susceptibility to drug abuse. There are no functional studies examining the acute signalling of MOPr-A6V in vitro, so we investigated potential functional differences between MOPr and MOPr-A6V at several signalling pathways using structurally distinct opioid ligands.

Experimental approach

CHO and AtT-20 cells stably expressing MOPr and MOPr-A6V were used. AC inhibition and ERK1/2 phosphorylation were assayed in CHO cells; K channel activation was assayed in AtT-20 cells.

Key

SUBMITTER: Knapman A 

PROVIDER: S-EPMC4403092 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature