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Abstract

Antagonist effects of beta-funaltrexamine and naloxonazine on alfentanil-induced antinociception and muscle rigidity in the rat.

S S Negus, G W Pasternak, G F Koob and M B Weinger
Journal of Pharmacology and Experimental Therapeutics February 1993, 264 (2) 739-745;
S S Negus
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G W Pasternak
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G F Koob
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M B Weinger
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Abstract

Alfentanil is a potent and short-acting mu opioid agonist that produces both antinociceptive effects and muscle rigidity. In the present study, the susceptibility of alfentanil-induced antinociception and rigidity to antagonism by the selective mu antagonist beta-funaltrexamine and the selective mu-1 antagonist naloxonazine was examined. Alfentanil (37.7-150.0 micrograms/kg) produced a dose-dependent increase both in antinociception as measured by the warm-water tail-dip assay and in rigidity as measured by electromyographic recording of the gastrocnemius muscle. Both beta-funaltrexamine (10.0 and 20.0 mg/kg) and naloxonazine (7.5 and 15.0 mg/kg) produced dose-dependent and parallel rightward shifts in the alfentanil dose-effect curves for both antinociception and rigidity. Furthermore, the alfentanil dose-effect curves for antinociception and rigidity were shifted to the right to a similar degree by any given pretreatment. These results suggest that alfentanil-induced antinociception in the warm-water tail-dip test and rigidity are mediated by pharmacologically similar populations of opioid receptors. More specifically, these results suggest that mu-1 opioid receptors mediate both alfentanil-induced antinociception and rigidity.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 264, Issue 2
1 Feb 1993
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Abstract

Antagonist effects of beta-funaltrexamine and naloxonazine on alfentanil-induced antinociception and muscle rigidity in the rat.

S S Negus, G W Pasternak, G F Koob and M B Weinger
Journal of Pharmacology and Experimental Therapeutics February 1, 1993, 264 (2) 739-745;

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Abstract

Antagonist effects of beta-funaltrexamine and naloxonazine on alfentanil-induced antinociception and muscle rigidity in the rat.

S S Negus, G W Pasternak, G F Koob and M B Weinger
Journal of Pharmacology and Experimental Therapeutics February 1, 1993, 264 (2) 739-745;
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