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Related Experiment Videos

The opioid ketobemidone has a NMDA blocking effect

S Andersen1, A H Dickenson, M Kohn

  • 1Department of Anaesthesiology, Hvidovre University Hospital, Denmark.

Pain
|October 1, 1996
PubMed
Summary

Ketobemidone effectively treats neurogenic pain through both opioid and non-opioid mechanisms. It reduces C-fiber responses and blocks N-methyl-D-aspartate (NMDA) receptor activation, unlike morphine.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Pain Research

Background:

  • Clinical observations suggest ketobemidone is effective for neurogenic pain, unlike pethidine and morphine.
  • This suggests ketobemidone may have both opioid and non-opioid analgesic effects.

Purpose of the Study:

  • To investigate the dual mechanism of action for ketobemidone in treating neurogenic pain.
  • To evaluate the opioid and non-opioid effects of ketobemidone on spinal cord neurons.

Main Methods:

  • Single unit recordings of dorsal horn neurons in anesthetized rats.
  • Measurement of neuronal responses to C-fiber stimulation and N-methyl-D-aspartate (NMDA) receptor activation.
  • Inhibition of [3H]MK-801 binding to assess NMDA receptor antagonism.

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Main Results:

  • Ketobemidone dose-dependently reduced C-fiber evoked responses.
  • Ketobemidone blocked neuronal wind-up more effectively than morphine, in a non-naloxone-reversible manner.
  • Ketobemidone inhibited [3H]MK-801 binding, indicating NMDA receptor antagonism.

Conclusions:

  • Ketobemidone exhibits both mu-opioid agonist and NMDA receptor antagonist properties.
  • These dual actions likely contribute to its efficacy in treating neurogenic pain.
  • Ketobemidone's non-naloxone-reversible NMDA antagonism differentiates it from morphine.