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Related Experiment Videos

Clocinnamox: a novel, systemically-active, irreversible opioid antagonist.

S D Comer1, T F Burke, J W Lewis

  • 1Department of Psychology, University of Michigan, Ann Arbor.

The Journal of Pharmacology and Experimental Therapeutics
|September 1, 1992
PubMed
Summary

Clocinnamox (C-CAM) acts as a long-lasting opioid antagonist in mice, suggesting a nonequilibrium mechanism. This novel mu opioid antagonist demonstrates prolonged effects compared to naltrexone.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Analgesia

Background:

  • Opioid agonists like morphine and fentanyl are used for pain relief.
  • Naltrexone is a standard opioid antagonist used to study opioid receptor mechanisms.

Purpose of the Study:

  • To investigate the analgesic effects of morphine and fentanyl in mice.
  • To characterize the antagonist properties of clocinnamox (C-CAM) at mu opioid receptors.

Main Methods:

  • Utilized the warm water tail-withdrawal assay in mice to measure analgesia.
  • Administered morphine, fentanyl, naltrexone, and C-CAM at various doses.
  • Determined dose-effect curves and antagonist pA2 values.

Main Results:

  • Both morphine and fentanyl produced dose-dependent analgesia, antagonized by naltrexone.

Related Experiment Videos

  • C-CAM shifted dose-effect curves and, at high doses, reduced maximal analgesic response.
  • C-CAM exhibited prolonged antagonism of morphine analgesia (up to 8 days) compared to naltrexone (2 days).
  • Fentanyl appeared more efficacious than morphine based on C-CAM dose requirements for maximal antagonism.

    • Conclusions:

    • C-CAM acts as a potent opioid antagonist with a long duration of action.
    • The prolonged antagonism suggests C-CAM may act via a nonequilibrium mechanism at opioid receptors.