Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands.

ABSTRACT: The present study investigated the in vitro pharmacology of the human kappa opioid receptor using multiple assays, including calcium mobilization in cells expressing chimeric G proteins, the dynamic mass redistribution (DMR) label-free assay, and a bioluminescence resonance energy transfer (BRET) assay that allows measurement of receptor interaction with G protein and β-arrestin 2. In all assays, dynorphin A, U-69,593, and [D-Pro¹⁰]dyn(1-11)-NH₂ behaved as full agonists with the following rank order of potency [D-Pro¹⁰]dyn(1-11)-NH₂ > dynorphin A ≥ U-69,593. [Dmt¹,Tic²]dyn(1-11)-NH₂ behaved as a moderate potency pure antagonist in the kappa-β-arrestin 2 interaction assay and as low efficacy partial agonist

SUBMITTER: Sturaro C 

PROVIDER: S-EPMC9068900 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature