TREK1 channel activation as a new analgesic strategy devoid of opioid adverse effects.

ABSTRACT:

Background and purpose

Opioids are effective painkillers. However, their risk-benefit ratio is dampened by numerous adverse effects and opioid misuse has led to a public health crisis. Safer alternatives are required, but isolating the antinociceptive effect of opioids from their adverse effects is a pharmacological challenge because activation of the μ opioid receptor triggers both the antinociceptive and adverse effects of opioids.

Experimental approach

The TREK1 potassium channel is activated downstream of μ receptor and involved in the antinociceptive activity of morphine but not in its adverse effects. Bypassing the μ opioid receptor to directly activate TREK1 could therefore be a safer analgesic strategy.

Key results

We developed a selective TREK1 activator, RNE

SUBMITTER: Busserolles J 

PROVIDER: S-EPMC7520446 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature