[HTML][HTML] Long-acting κ opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase
MR Bruchas, T Yang, S Schreiber, M DeFino… - Journal of Biological …, 2007 - ASBMB
Norbinaltorphimine (NorBNI), guanidinonaltrindole, and atrans-(3R, 4R)-dimethyl-4-(3-
hydroxyphenyl) piperidine (JDTic) are selective κ opioid receptor (KOR) antagonists having
very long durations of action in vivo despite binding non-covalently in vitro and having only
moderately high affinities. Consistent with this, we found that antagonist treatment
significantly reduced the subsequent analgesic response of mice to the KOR agonist U50,
488 in the tail-withdrawal assay for 14–21 days. Receptor protection assays were designed …
hydroxyphenyl) piperidine (JDTic) are selective κ opioid receptor (KOR) antagonists having
very long durations of action in vivo despite binding non-covalently in vitro and having only
moderately high affinities. Consistent with this, we found that antagonist treatment
significantly reduced the subsequent analgesic response of mice to the KOR agonist U50,
488 in the tail-withdrawal assay for 14–21 days. Receptor protection assays were designed …