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Related Experiment Videos

Opioid peptide-derived analgesics.

Peter W Schiller1

  • 1Laboratory of Chemical Biology and Peptide Research, Clinical Research Institute of Montreal, Quebec, Canada H2W 1R7. schillp@ircm.qc.ca

The AAPS Journal
|December 16, 2005
PubMed
Summary
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New opioid peptides show promise as potent analgesics with reduced side effects. [Dmt(1)]DALDA offers strong pain relief and crosses the blood-brain barrier, while mixed mu agonist/delta antagonists may reduce tolerance and dependence.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Neuroscience

Background:

  • Opioid peptides are crucial for pain management.
  • Developing novel analgesics with improved efficacy and safety profiles is a priority.
  • Existing analgesics like morphine have limitations, including tolerance and dependence.

Purpose of the Study:

  • To review recent advancements in opioid peptide-based analgesics.
  • To evaluate the analgesic potential and properties of dermorphin-derived tetrapeptide [Dmt(1)]DALDA.
  • To explore the development of mixed mu agonist/delta antagonists as novel analgesic candidates.

Main Methods:

  • In vitro receptor binding assays to determine affinity and selectivity.
  • In vivo analgesic assays (tail-flick test) in mice and rats.

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  • Assessment of antinociceptive effects, duration of action, and respiratory function.
  • Evaluation of blood-brain barrier penetration and cross-tolerance with morphine.
  • Characterization of mu agonist/delta antagonist profile and dependence liability.

    • Main Results:

    • [Dmt(1)]DALDA exhibits subnanomolar mu receptor affinity, high selectivity, and potent in vitro agonist activity.
    • [Dmt(1)]DALDA demonstrates extraordinary antinociceptive effects and long duration in vivo, crossing the blood-brain barrier with minimal respiratory impact.
    • Little cross-tolerance was observed between [Dmt(1)]DALDA and morphine.
    • The mixed mu agonist/delta antagonist DIPP-NH(2)[Psi] shows promising in vitro and in vivo (central administration) analgesic effects with reduced physical dependence and tolerance compared to morphine.

    Conclusions:

    • [Dmt(1)]DALDA represents a potent analgesic with favorable properties, including systemic activity and reduced cross-tolerance.
    • Mixed mu agonist/delta antagonists, exemplified by DIPP-NH(2)[Psi], hold potential for developing analgesics with lower tolerance and dependence liabilities.
    • Further development is needed to identify systemically active mixed mu agonist/delta antagonists for clinical use.