Differential effects of systemically administered nor-binaltorphimine (nor-BNI) on κ-opioid agonists in the mouse writhing assay
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منابع مشابه
Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
BACKGROUND Nor-BNI, GNTI and JDTic induce κ opioid antagonism that is delayed by hours and can persist for months. Other effects are transient. It has been proposed that these drugs may be slowly absorbed or distributed, and may dissolve in cell membranes, thus slowing elimination and prolonging their effects. Recent evidence suggests, instead, that they induce prolonged desensitization of the ...
متن کاملSelective κ Opioid Antagonists nor-BNI, GNTI and JDTic Have Low Affinities for Non-Opioid Receptors and Transporters
BACKGROUND Nor-BNI, GNTI and JDTic induce selective κ opioid antagonism that is delayed and extremely prolonged, but some other effects are of rapid onset and brief duration. The transient effects of these compounds differ, suggesting that some of them may be mediated by other targets. RESULTS In binding assays, the three antagonists showed no detectable affinity (K(i)≥10 µM) for most non-opi...
متن کاملPhysical presence of nor-binaltorphimine in mouse brain over 21 days after a single administration corresponds to its long-lasting antagonistic effect on κ-opioid receptors.
In the mouse 55°C warm-water tail-withdrawal assay, a single administration of nor-binaltorphimine (nor-BNI; 10 mg/kg i.p.) antagonized κ-opioid receptor (KOR) agonist-induced antinociception up to 14 days, whereas naloxone (10 mg/kg i.p.)-mediated antagonism lasted less than 1 day. In saturation binding experiments, mouse brain membranes isolated and washed 1 or 7 (but not 14) days after nor-B...
متن کاملnor-BNI Antagonism of Kappa Opioid Agonist-Induced Reinstatement of Ethanol-Seeking Behavior
Recent work suggests that the dynorphin (DYN)/kappa opioid receptor (KOR) system may be a key mediator in the behavioral effects of alcohol. The objective of the present study was to examine the ability of the KOR antagonist norbinaltorphimine (nor-BNI) to attenuate relapse to ethanol seeking due to priming injections of the KOR agonist U50,488 at time points consistent with KOR selectivity. Ma...
متن کاملCentral kappa-opioid receptor-mediated antidepressant-like effects of nor-Binaltorphimine: behavioral and BDNF mRNA expression studies.
kappa-opioid receptor antagonists such as nor-Binaltorphimine (nor-BNI) have been shown to produce antidepressant-like behavioral effects in animal models of depression. The aim of this study was to investigate further the duration of centrally administered nor-BNI-induced antidepressant-like actions measured by both behavior and brain-derived neurotrophic factor (BDNF) gene expression. In addi...
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ژورنال
عنوان ژورنال: Psychopharmacology
سال: 1994
ISSN: 0033-3158,1432-2072
DOI: 10.1007/bf02245071