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- W1973380329 abstract "Tyr-d-Ala-Gly-Phe-d-Nle-Arg-Phe (DADN) a synthetic analogue of the endogenous Met-enkephalin-Arg-Phe (Tyr-Gly-Gly-Phe-Met-Arg-Phe; MERF), was investigated in radioligand binding assays, [35S]GTPγS stimulation experiments as well as in in vivo algesiometric tests. Binding properties of [3H]DADN were measured in crude membrane fractions of rat spinal cord tissues and in homogenates of Chinese hamster ovary (CHO) cells selectively expressing δ-, κ-or μ-opioid receptors. The highest affinity for [3H]DADN binding was observed in membranes from CHO cells transfected with μ-opioid receptors confirming the μ-selectivity of the peptide. Unlabeled DADN was also investigated in functional biochemical experiments by measuring opioid receptor-mediated G-protein activation in rat brain membrane fractions. The peptide stimulated the activity of the regulatory G-proteins in a concentration dependent manner, and the stimulation was efficiently inhibited in the presence of μ-receptor specific antagonist ligands further supporting the selectivity profile of DADN. Intrathecally administered DADN produced a dose-related, naloxone-reversible antinociception in rat hot water tail-flick tests. Among the selective opioid antagonists tested, the δ-selective naltrindole (NTI) and the κ-specific norbinaltorphimine (norBNI) showed only slight blocking effects compared with naloxone. The results obtained in the in vitro agonist-stimulated [35S]GTPγS binding assays are in good agreement with the opioid agonist effect seen in the in vivo pain test." @default.
- W1973380329 created "2016-06-24" @default.
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- W1973380329 date "2004-10-01" @default.
- W1973380329 modified "2023-10-10" @default.
- W1973380329 title "Pharmacological and functional biochemical properties of d-Ala2-d-Nle5-enkephalin-Arg-Phe" @default.
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- W1973380329 doi "https://doi.org/10.1016/j.regpep.2004.06.017" @default.
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