Abstract |
The antinociceptive effect of i.v. kelatorphan (2.5, 5, 10 and 15 mg/kg), a mixed inhibitor of enkephalin degrading enzymes, was studied in a rat model of peripheral unilateral mononeuropathy (chronic constriction of the common sciatic nerve). Kelatorphan at 2.5 and 5 mg/kg had no significant effect on the vocalization threshold to paw pressure test, but higher doses (10 mg/kg) produced a significant antinociceptive effect which plateaued at 15 mg/kg, on both hindpaws. Kelatorphan (10 mg/kg) was co-injected with the specific mu-, delta- and kappa-opioid receptor antagonists naloxone (0.1 mg/kg), naltrindole (1 mg/kg) or nor-binaltorphimine (1 mg/kg). The effect of kelatorphan 10 mg/kg was completely prevented by naloxone, reduced by 75% by naltrindole (both hindpaws), and reduced by 50% by nor-binaltorphimine (contralateral paw only).
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Authors | S H Lee, V Kayser, G Guilbaud |
Journal | European journal of pharmacology
(Eur J Pharmacol)
Vol. 264
Issue 1
Pg. 61-7
(Oct 13 1994)
ISSN: 0014-2999 [Print] Netherlands |
PMID | 7828644
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Analgesics
- Dipeptides
- Receptors, Opioid
- kelatorphan
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Topics |
- Analgesics
(pharmacology)
- Animals
- Dipeptides
(antagonists & inhibitors, pharmacology)
- Disease Models, Animal
- Male
- Nociceptors
(drug effects)
- Pain
(drug therapy, etiology, physiopathology)
- Pain Measurement
- Peripheral Nervous System Diseases
(physiopathology)
- Rats
- Rats, Sprague-Dawley
- Receptors, Opioid
(drug effects)
- Sciatic Nerve
(physiology)
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