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Blockade of the antinociceptive activity of centrally administered ketorolac by nor-binaltorphimine.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1995 May 04; Vol. 278 (1), pp. 27-32. - Publication Year :
- 1995
-
Abstract
- Antinociceptive activity of intracerebroventricularly administered ketorolac tromethamine was evaluated in mice by measuring inhibition of abdominal stretching induced by p-phenylquinone. Ketorolac tromethamine produced dose-dependent antinociception with an ED50 of 7.34 micrograms/mouse (4.97-10.82) and a maximal effect at 30 micrograms. Selective antagonists of opioid receptors were used to determine ketorolac's mechanism of action. The ketorolac tromethamine-induced antinociception was not blocked by the mu- and delta-opioid receptor antagonists, naloxone and ICI-174,864 (N,N-diallyl-Tyr-Aib-Aib-Phe-Leu), respectively; however, the kappa-opioid receptor antagonist nor-binaltorphimine dihydrochloride significantly blocked this effect. These findings suggest that activation of kappa-opioid receptors appears to play a role in the mechanism of the antinociceptive effect of ketorolac tromethamine. Ketorolac tromethamine may induce the release of endogenous kappa-opioids to produce central nervous system antinociception.
- Subjects :
- Analgesia
Analgesics, Non-Narcotic administration & dosage
Analgesics, Non-Narcotic toxicity
Analysis of Variance
Animals
Benzoquinones pharmacology
Dose-Response Relationship, Drug
Drug Interactions
Enkephalin, Leucine administration & dosage
Enkephalin, Leucine analogs & derivatives
Enkephalin, Leucine pharmacology
Injections, Intraventricular
Ketorolac Tromethamine
Male
Mice
Mice, Inbred ICR
Naloxone administration & dosage
Naloxone pharmacology
Naltrexone administration & dosage
Naltrexone pharmacology
Narcotic Antagonists administration & dosage
Narcotic Antagonists pharmacology
Receptors, Opioid, delta drug effects
Receptors, Opioid, delta metabolism
Receptors, Opioid, kappa drug effects
Receptors, Opioid, kappa metabolism
Receptors, Opioid, mu drug effects
Receptors, Opioid, mu metabolism
Tolmetin administration & dosage
Tolmetin antagonists & inhibitors
Tolmetin toxicity
Tromethamine administration & dosage
Tromethamine toxicity
Analgesics, Non-Narcotic antagonists & inhibitors
Naltrexone analogs & derivatives
Tolmetin analogs & derivatives
Tromethamine analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 278
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 7664811
- Full Text :
- https://doi.org/10.1016/0014-2999(95)00091-x