In vitro and in vivo characterization of the bifunctional μ and δ opioid receptor ligand UFP-505.

ABSTRACT:

Background and purpose

Targeting more than one opioid receptor type simultaneously may have analgesic advantages in reducing side-effects. We have evaluated the mixed μ opioid receptor agonist/ δ opioid receptor antagonist UFP-505 in vitro and in vivo.

Experimental approach

We measured receptor density and function in single μ, δ and μ /δ receptor double expression systems. GTPγ³⁵ S binding, cAMP formation and arrestin recruitment were measured. Antinociceptive activity was measured in vivo using tail withdrawal and paw pressure tests following acute and chronic treatment. In some experiments, we collected tissues to measure receptor densities.

Key results

UFP-505 bound to μ receptors with full agonist activity and to δ receptors as a low efficacy partial a

SUBMITTER: Dietis N 

PROVIDER: S-EPMC6016625 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature