Human native kappa opioid receptor functions not predicted by recombinant receptors: Implications for drug design.

ABSTRACT: If activation of recombinant G protein-coupled receptors in host cells (by drugs or other ligands) has predictive value, similar data must be obtained with native receptors naturally expressed in tissues. Using mouse and human recombinant κ opioid receptors transfected into a host cell, two selectively-acting compounds (ICI204448, asimadoline) equi-effectively activated both receptors, assessed by measuring two different cell signalling pathways which were equally affected without evidence of bias. In mouse intestine, naturally expressing κ receptors within its nervous system, both compounds also equi-effectively activated the receptor, inhibiting nerve-mediated muscle contraction. However, whereas ICI204448 acted similarly in human intestine, where κ receptors are again expressed within i

SUBMITTER: Broad J 

PROVIDER: S-EPMC4974614 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature