Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration

J Med Chem. 1999 Feb 11;42(3):400-4. doi: 10.1021/jm9810699.

Abstract

In the present paper we describe the synthesis of some dermorphin and deltorphin analogues beta-O- and alpha-C-glycosylated on the C-terminal amino acid residue and report their opioid receptor affinity and selectivity as well as their analgesic potency after subcutaneous injection in mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Analgesics, Opioid / chemical synthesis*
  • Analgesics, Opioid / chemistry
  • Analgesics, Opioid / pharmacology
  • Animals
  • Glycosylation
  • Guinea Pigs
  • In Vitro Techniques
  • Injections, Subcutaneous
  • Male
  • Mice
  • Muscle, Smooth / drug effects
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology
  • Opioid Peptides
  • Receptors, Opioid / drug effects

Substances

  • Analgesics, Opioid
  • Oligopeptides
  • Opioid Peptides
  • Receptors, Opioid
  • deltorphin
  • dermorphin