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Molecular Pharmacology

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Research ArticleArticle

Inhibition of Drug Metabolism

II. Metabolism of 2-Diethylaminoethyl 2,2-Diphenylvalerate HCI (SKF 525-A)

M. W. ANDERS, A. P. ALVARES and G. J. MANNERING
Molecular Pharmacology July 1966, 2 (4) 328-334;
M. W. ANDERS
Department of Pharmacology, University of Minnesota, Minneapolis, Minnesota 55455
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A. P. ALVARES
Department of Pharmacology, University of Minnesota, Minneapolis, Minnesota 55455
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G. J. MANNERING
Department of Pharmacology, University of Minnesota, Minneapolis, Minnesota 55455
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Abstract

The metabolism of SKF 525-A by washed hepatic microsomes from the rat was studied. The secondary amine derivative, 2-ethylaminoethyl 2,2-diphenylvalerate HCl (SKF 8742-A) was identified as a metabolite. A second metabolite, designated metabolite I, was also observed. The acidic hydrolysis product of SKF 525-A, 2,2-diphenylvalerate (SKF 2314), was identified and the rate of hydrolysis of SKF 525-A by washed microsomes was measured. Metabolite I was not found in microsomal preparations that had been incubated with SKF 8742-A. No SKF 525-A or SKF 8742-A was recovered from the urine, bile, or feces of rats that had received these compounds, nor were metabolites found in these materials. The primary amine analog of SKF 525-A, 2-aminoethyl 2,2-diphenylvalerate hydrobromide (AEDV) was synthesized. AEDV was shown to be a competitive inhibitor of the N-demethylation of ethylmorphine with an inhibition constant quite similar to those of SKF 525-A and SKF 8742-A.

ACKNOWLEDGMENTS This research was supported by USPHS grant No. GM-12543. Part of this material appears in a thesis by M. W. Anders in partial fulfillment of time requirements for the Ph.D. degree in the Department of Pharmacology, University of Minnesota, 1964. The authors gratefully acknowledge the able technical assistance of Mr. Donald W. Shoeman and Mrs. Sheila Ham. We are grateful to Dr. Philip S. Portoghese for his helpful suggestions regarding the synthesis of AEDV.

  • Copyright ©, 1966, by Academic Press Inc.

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Molecular Pharmacology
Vol. 2, Issue 4
1 Jul 1966
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Research ArticleArticle

Inhibition of Drug Metabolism

M. W. ANDERS, A. P. ALVARES and G. J. MANNERING
Molecular Pharmacology July 1, 1966, 2 (4) 328-334;

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Research ArticleArticle

Inhibition of Drug Metabolism

M. W. ANDERS, A. P. ALVARES and G. J. MANNERING
Molecular Pharmacology July 1, 1966, 2 (4) 328-334;
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