Potent antinociceptive effects of Kelatorphan (a highly efficient inhibitor of multiple enkephalin-degrading enzymes) systemically administered in normal and arthritic rats

@article{Kayser1989PotentAE,
  title={Potent antinociceptive effects of Kelatorphan (a highly efficient inhibitor of multiple enkephalin-degrading enzymes) systemically administered in normal and arthritic rats},
  author={Val{\'e}rie Kayser and M. -C. Fourni{\'e}-Zaluski and Gis{\'e}le Guilbaud and B. Roques},
  journal={Brain Research},
  year={1989},
  volume={497},
  pages={94-101}
}
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79 Citations
Background Citations
9
Methods Citations
3
Results Citations
1

79 Citations

Antinociceptive effect of systemic PC 12, a prodrug mixed inhibitor of enkephalin-degrading enzymes, in normal and arthritic rats.
Antinociceptive effect of systemic kelatorphan, in mononeuropathic rats, involves different opioid receptor types.
Potent antinociceptive effects of clonidine systemically administered in an experimental model of clinical pain, the arthritic rat
The highly selective δ agonist BUBU induces an analgesic effect in normal and arthritic rat and this action is not affected by repeated administration of low doses of morphine
Antinociceptive response induced by mixed inhibitors of enkephalin catabolism in peripheral inflammation
Effects of the analgesic agent tramadol in normal and arthritic rats: comparison with the effects of different opioids, including tolerance and cross-tolerance to morphine.
Antinociceptive effects of RB101, a complete inhibitor of enkephalin-catabolizing enzymes, are enhanced by a cholecystokinin type B receptor antagonist, as revealed by noxiously evoked spinal c-Fos expression in rats.
TLDR
Results show that RB101 dose-dependently decreases carrageenin-evoked spinal c-Fos expression, and the effectiveness of RB101 can be revealed by preadministration of the CCK(B) receptor antagonist CI988.
Analgesic responses elicited by endogenous enkephalins (protected by mixed peptidase inhibitors) in a variety of morphine-sensitive noxious tests.
Behavioural evidence for a peripheral component in the enhanced antinociceptive effect of a low dose of systemic morphine in carrageenin-induced hyperalgesic rats
The effects of RB101, a mixed inhibitor of enkephalin-catabolizing enzymes, on carrageenin-induced spinal c-Fos expression are completely blocked by β-funaltrexamine, a selective μ-opioid receptor antagonist
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References

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The analgesic effects of morphine, but not those of the enkephalinase inhibitor thiorphan, are enhanced in arthritic rats
Analgesic effects of kelatorphan, a new highly potent inhibitor of multiple enkephalin degrading enzymes.
Effects of kelatorphan and other peptidase inhibitors on the in vitro and in vivo release of methionine-enkephalin-like material from the rat spinal cord.
TLDR
Compared to thiorphan plus bestatin, kelatorphan exerts additional inhibitory effects on dipeptidylaminopeptidase activity and the present results could indicate that this enzyme also may be involved in the inactivation of extracellular Met-enkephalin at the spinal level in rats.
In vitro and in vivo effects of kelatorphan on enkephalin metabolism in rodent brain.
Opioid receptor types and antinociceptive activity in chronic inflammation: bothe κ- and μ-opiate agonistic effects are enhanced in arthritic rats
Differential effects of various doses of morphine and naloxone on two nociceptive test thresholds in arthritic and normal rats
Prevention of degradation of endogenous enkephalins produces inhibition of nociceptive neurones in rat spinal cord
Enkephalinase a activity in different regions of brain and spinal cord of normal and chronic arthritic rats
Functional Response of Multiple Opioid Systems to Chronic Arthritic Pain in the Rat a
TLDR
In evaluating the relationship between opioid systems and nociceptive processing, it is imperative to take into account their multiplicity, which includes a multiplicity of opioid ligands and opioid receptors that display a differential distribution and modulation and appear to subserve.
Reaction thresholds to pressure in edematous hindpaws of rats and responses to analgesic drugs.
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TLDR
In their effects in this test, the narcotic antagonists resemble nonnarcotic analgesics.
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