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International Union of Pharmacology. XII. Classification of opioid receptors.
The results show that data from published knowledge can be used to provide reliable, patient level, automated risk assessment, potentially reducing the cognitive burden on physicians and helping policy makers better prepare for future needs. Expand
Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats.
Findings are consistent with the hypothesis that CREB-mediated induction of dynorphin in the NAc "triggers" immobility behavior in the FST and raise the possibility that kappa-antagonists may have efficacy as antidepressants, but lack stimulant or reward-related effects. Expand
Antidepressant-Like Effects of κ-Opioid Receptor Antagonists in the Forced Swim Test in Rats
We showed previously that cAMP response element-binding protein (CREB) within the nucleus accumbens (NAc) of rats regulates immobility in the forced swim test (FST), an assay used to studyExpand
Safety assessment of allylalkoxybenzene derivatives used as flavouring substances - methyl eugenol and estragole.
Present exposure to methyl eugenol and estragole resulting from consumption of food, mainly spices and added as such, does not pose a significant cancer risk. Expand
Binaltorphimine and nor-binaltorphimine, potent and selective kappa-opioid receptor antagonists.
BNI and nor-BNI represent the first highly selective kappa opioids receptor antagonists and should be of great utility as molecular probes for identifying the interaction of agonist ligands with kappa opioid receptors in vitro and in vivo. Expand
Nor-binaltorphimine, a highly selective kappa-opioid antagonist in analgesic and receptor binding assays.
Nor-BNI and U-50,488H were used to demonstrate that kappa opioid receptors in the spinal cord were more important than those located supraspinally for kappa-mediated analgesia and the comparatively low selectivity of BNI in receptor binding studies did not correlate with the high pharmacologic selectivity for k Kappa receptors. Expand
A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers.
This study demonstrates a proof of concept for tissue-selective drug targeting based on G protein-coupled receptor heterodimerization and shows that the opioid agonist ligand 6'-guanidinonaltrindole (6'-GNTI) has the unique property of selectively activating only opioid receptorheterodimers but not homomers. Expand
Opioid-induced tolerance and dependence in mice is modulated by the distance between pharmacophores in a bivalent ligand series.
Data suggest that physical interaction between the mu and delta opioid receptors modulates mu-mediated tolerance and dependence, and offers a previously uncharacterized approach for the development of analgesics devoid ofolerance and dependence. Expand