Engineering endomorphin drugs: state of the art

  title={Engineering endomorphin drugs: state of the art},
  author={L. Lazarus and Y. Okada},
  journal={Expert Opinion on Therapeutic Patents},
  pages={1 - 14}
  • L. Lazarus, Y. Okada
  • Published 2012
  • Chemistry, Medicine
  • Expert Opinion on Therapeutic Patents
Introduction: Although endomorphins-1 (EM-1; H-Tyr-Pro-Phe-Trp-NH2) and -2 (EM-2; H-Tyr-Pro-Phe-Phe-NH2) are primarily considered agonists for the μ-opioid receptor (MOR), systematic alterations to specific residues provided antagonists and ligands with mixed μ/δ-opioid properties, suitable for application to health-related topics. While the application of endomorphins as antinociceptive agents and numerous biological endpoints were experimentally delineated in laboratory animals and in vitro… Expand
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Endomorphin-1 Analogues Containing β-Proline Are μ-Opioid Receptor Agonists and Display Enhanced Enzymatic Hydrolysis Resistance
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