43
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: not found

      Glycopeptide enkephalin analogues produce analgesia in mice: evidence for penetration of the blood-brain barrier.

      Proceedings of the National Academy of Sciences of the United States of America
      Amino Acid Sequence, Analgesics, pharmacokinetics, pharmacology, Animals, Biological Transport, Blood-Brain Barrier, Enkephalins, Glycopeptides, Mice, Molecular Sequence Data

      Read this article at

      ScienceOpenPublisherPMC
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          Most peptides have not proved useful as neuroactive drugs because they are blocked by the blood-brain barrier and do not reach their receptors within the brain. Intraperitoneally administered L-serinyl beta-D-glucoside analogues of [Met5]enkephalin (glycopeptides) have been shown to be transported across the blood-brain barrier to bind with targeted mu- and delta-opioid receptors in the mouse brain. The opioid nature of the binding has been demonstrated with intracerebroventricularly administered naloxone. Paradoxically, glucosylation decreases the lipophilicity of the peptides while promoting transport across the lipophilic endothelial layer. It is suggested that glucose transporter GLUT-1 is responsible for the transport of the peptide message. Profound and long-lasting analgesia has been observed in mice (tail-flick and hot-plate assays) with two of the glycopeptide analogues when administered intraperitoneally.

          Related collections

          Author and article information

          Journal
          8041755
          44349
          10.1073/pnas.91.15.7114

          Chemistry
          Amino Acid Sequence,Analgesics,pharmacokinetics,pharmacology,Animals,Biological Transport,Blood-Brain Barrier,Enkephalins,Glycopeptides,Mice,Molecular Sequence Data

          Comments

          Comment on this article