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Molecular Pharmacology

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Research ArticleArticle

The Interaction of Phenoxybenzamine with the Mouse Brain Opiate Receptor

VINA SPIEHLER, ALAN S. FAIRHURST and LOWELL O. RANDALL
Molecular Pharmacology July 1978, 14 (4) 587-595;
VINA SPIEHLER
Department of Medical Pharmacology and Therapeutics, University of California College of Medicine, Irvine, California 92717
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ALAN S. FAIRHURST
Department of Medical Pharmacology and Therapeutics, University of California College of Medicine, Irvine, California 92717
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LOWELL O. RANDALL
Department of Medical Pharmacology and Therapeutics, University of California College of Medicine, Irvine, California 92717
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Abstract

Phenoxybenzamine was found to displace stereospecifically bound [3H]naloxone from mouse brain homogenates in a dose-related manner, with an IC50 of 4.6 µM. In the presence of 100 mM Na+, the dose-response curve shifted to give an IC50 of 19 µM and an Na+ response ratio of 4.3, which is similar to that of a mixed agonist-antagonist. Scatchard plots of the binding data showed that phenoxybenzamine reduced the number of receptor binding sites for naloxone but did not change the affinity of the unreacted receptors for naloxone. Levallorphan protected the receptor from phenoxybenzamine, but the inhibition of binding activity produced by phenoxybenzamine could not be reversed by repeated washing of the receptor preparation. It thus appears that phenoxybenzamine acts as an irreversible, non-equilibrium inhibitor with binding characteristics similar to those of the agonist-antagonist narcotics. Washed brain homogenates from mice treated in vivo with antinociceptive doses of phenoxybenzamine exhibited enhanced binding of [3H]naloxone and [3H]morphine, which may indicate the displacement of an endogenous material from the opiate receptors in vivo by phenoxybenzamine.

  • Copyright © 1978 by Academic Press, Inc.

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Molecular Pharmacology
Vol. 14, Issue 4
1 Jul 1978
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Research ArticleArticle

The Interaction of Phenoxybenzamine with the Mouse Brain Opiate Receptor

VINA SPIEHLER, ALAN S. FAIRHURST and LOWELL O. RANDALL
Molecular Pharmacology July 1, 1978, 14 (4) 587-595;

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Research ArticleArticle

The Interaction of Phenoxybenzamine with the Mouse Brain Opiate Receptor

VINA SPIEHLER, ALAN S. FAIRHURST and LOWELL O. RANDALL
Molecular Pharmacology July 1, 1978, 14 (4) 587-595;
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