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KMID : 0043319950180060381
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Archives of Pharmacal Research
1995 Volume.18 No. 6 p.381 ~ p.384
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In vitro Ccovalent Binding of SC-42867, PGE2 Antagonist, to Rat Liver Microsomal Proteins
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Lee Kyung-Tae
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Abstract
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Covalent binding of the reactive metabolites of SC_42867 to microsomal proteins has been examined. In the absence of inhibitor of cytochrome oxydase (.alpha.-naphtyl-isothiocyanate) or a radical scavenger (3-terthiobuty-4-hydroxyanisol), up to 4.0% of total redioactivity used in the assay could irreversibly bind to proteins. In the presence of an inhibitor, the highest percentage of covalent binding observed is 0.7% a significant decrease of the metabolism of SC42876 was observed. These results suggest in a cytochrome P-450 dependent generation of SC_42867 metabolites significantly take part in the covalent binding process.
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KEYWORD
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Covalent binding, Liver microsomes, Cytochrom p-450
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