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Blockade of the antinociceptive activity of centrally administered ketorolac by nor-binaltorphimine.

Authors :
Tripathi A
Welch SP
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.

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