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Phosphorylation of l‐serine‐containing enkephalin analogs has been explored as an alternative to glycosylation in an effort to increase blood–brain barrier permeability and CNS bioavailability of peptide pharmacophores. Two enkephalin‐based peptides were modified for these studies, a set related to DTLES, a mixed μ/δ‐agonist, and one related to DAMGO, a highly selective μ‐agonist. Each unglycosylated...
The current study assessed the in vivo antagonist properties of nalmefene using procedures previously used to characterize the opioid antagonists naloxone, naltrexone, 6β-naltrexol and nalbuphine.ICR mice were used to generate antagonist dose–response curves with intraperitoneal (i.p.) nalmefene against fixed A 90 doses of morphine in models of morphine-stimulated hyperlocomotion and antinociception...
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