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[Effect of the lipophilic spin-labeled inhibitor of cytochrome P-450 on the activity of the microsomal system].

T N Subkhankulova, В В Ляхович, L. M. Vainer

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Abstract

It was shown that the lipophilic nitroxyl radical--2-hexyl-2,3,5,5-tetramethyl-4-(3-iodo-2-oxopropyliden)-im idazolidine- 1-oxyl, an affinity modified of rat liver microsomal cytochrome P-450, interacts with various forms of cytochrome P-450 as substrate type I, and it inhibits the oxidation of substrates specific for these forms. During its intravenous injection with egg phosphatidylcholine liposomes the radical is partly bound to liver microsomes, which is accompanied by a decrease of the oxygenase activity of microsomal preparations (by 30-50%) as well as by prolongation of the soporific effect of hexabarbital (2-3-fold).

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What this paper is about

It was shown that the lipophilic nitroxyl radical--2-hexyl-2,3,5,5-tetramethyl-4-(3-iodo-2-oxopropyliden)-im idazolidine- 1-oxyl, an affinity modified of rat liver microsomal cytochrome P-450, interacts with various forms of cytochrome P-450 as substrate type I, and it inhibits the oxidation of substrates specific for these forms. During its intravenous injection with egg phosphatidylcholine liposomes the radical is partly bound to liver microsomes, which is accompanied by a decrease of the oxygenase activity of microsomal preparations (by 30-50%) as well as by prolongation of the soporific effect of hexabarbital (2-3-fold).

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Available abstract

It was shown that the lipophilic nitroxyl radical--2-hexyl-2,3,5,5-tetramethyl-4-(3-iodo-2-oxopropyliden)-im idazolidine- 1-oxyl, an affinity modified of rat liver microsomal cytochrome P-450, interacts with various forms of cytochrome P-450 as substrate type I, and it inhibits the oxidation of substrates specific for these forms. During its intravenous injection with egg phosphatidylcholine liposomes the radical is partly bound to liver microsomes, which is accompanied by a decrease of the oxygenase activity of microsomal preparations (by 30-50%) as well as by prolongation of the soporific effect of hexabarbital (2-3-fold).

Key concepts: Microsome, Cytochrome, Chemistry, Phosphatidylcholine, Liposome, Nitroxyl, Cytochrome P450, Microsoma

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[Effect of the lipophilic spin-labeled inhibitor of cytochrome P-450 on the activity of the microsomal system]. — Research Paper | ScholarLens