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Molecular Pharmacology

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Research ArticleArticle

Studies of the Porphyrin-Inducing Activity of Ethynyl Compounds and Conformationally Restricted and Unrestricted Analogues of Allylisopropylacetamide in Chick Embryo Liver Cell Culture

GERALD S. MARKS, STEPHEN B. ZIMMER, STEPHEN E. DINIZO, BRUCE A. MICO, KENT L. KUNZE and PAUL R. ORTIZ DE MONTELLANO
Molecular Pharmacology July 1981, 20 (1) 206-210;
GERALD S. MARKS
Department of Pharmacology, Queen's University, Kingston, Ontario, Canada, K7L 3N6, and Department of Pharmaceutical Chemistry, School of Pharmacy and Liver Center, University of California, San Francisco, California 94143
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STEPHEN B. ZIMMER
Department of Pharmacology, Queen's University, Kingston, Ontario, Canada, K7L 3N6, and Department of Pharmaceutical Chemistry, School of Pharmacy and Liver Center, University of California, San Francisco, California 94143
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STEPHEN E. DINIZO
Department of Pharmacology, Queen's University, Kingston, Ontario, Canada, K7L 3N6, and Department of Pharmaceutical Chemistry, School of Pharmacy and Liver Center, University of California, San Francisco, California 94143
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BRUCE A. MICO
Department of Pharmacology, Queen's University, Kingston, Ontario, Canada, K7L 3N6, and Department of Pharmaceutical Chemistry, School of Pharmacy and Liver Center, University of California, San Francisco, California 94143
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KENT L. KUNZE
Department of Pharmacology, Queen's University, Kingston, Ontario, Canada, K7L 3N6, and Department of Pharmaceutical Chemistry, School of Pharmacy and Liver Center, University of California, San Francisco, California 94143
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PAUL R. ORTIZ DE MONTELLANO
Department of Pharmacology, Queen's University, Kingston, Ontario, Canada, K7L 3N6, and Department of Pharmaceutical Chemistry, School of Pharmacy and Liver Center, University of California, San Francisco, California 94143
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Abstract

A series of conformationally restricted and unrestricted analogues of allylisopropylacetamide (AIA) and a group of ethynyl compounds have been tested for porphyrin-inducing activity in chick embryo liver cell culture. The conformationally restricted analogues, which do not share the ability of AIA to destroy rat and chick embryo hepatic cytochrome P-450, were nevertheless shown to induce porphyrin accumulation. The conformationally unrestricted analogues and the ethynyl compounds which do share the ability of AIA to destroy rat hepatic cytochrome P-450 possessed weak to moderate porphyrin-inducing activity or were inactive. It is concluded that in chick embryo liver cell culture, in contrast to the situation in rat liver, destruction of the heme moiety of cytochrome P-450 does not appear to be a prerequisite for δ-aminolevulinic acid synthetase induction and porphyrin accumulation.

  • Copyright © 1981 by The American Society for Pharmacology and Experimental Therapeutics

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Molecular Pharmacology
Vol. 20, Issue 1
1 Jul 1981
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Research ArticleArticle

Studies of the Porphyrin-Inducing Activity of Ethynyl Compounds and Conformationally Restricted and Unrestricted Analogues of Allylisopropylacetamide in Chick Embryo Liver Cell Culture

GERALD S. MARKS, STEPHEN B. ZIMMER, STEPHEN E. DINIZO, BRUCE A. MICO, KENT L. KUNZE and PAUL R. ORTIZ DE MONTELLANO
Molecular Pharmacology July 1, 1981, 20 (1) 206-210;

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Research ArticleArticle

Studies of the Porphyrin-Inducing Activity of Ethynyl Compounds and Conformationally Restricted and Unrestricted Analogues of Allylisopropylacetamide in Chick Embryo Liver Cell Culture

GERALD S. MARKS, STEPHEN B. ZIMMER, STEPHEN E. DINIZO, BRUCE A. MICO, KENT L. KUNZE and PAUL R. ORTIZ DE MONTELLANO
Molecular Pharmacology July 1, 1981, 20 (1) 206-210;
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