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Abstract

Identification of cytochrome P-450 isozymes involved in the hydroxylation of dantrolene by rat liver microsomes.

Z Jayyosi, J Villoutreix, J M Ziegler, A M Batt, F De Maack, G Siest and P E Thomas
Drug Metabolism and Disposition September 1993, 21 (5) 939-945;
Z Jayyosi
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J Villoutreix
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J M Ziegler
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A M Batt
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F De Maack
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G Siest
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P E Thomas
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Abstract

The role of individual rat liver cytochrome P-450 isozymes in the metabolism of the skeletal muscle relaxant, dantrolene, was studied. Following incubation of dantrolene with hepatic microsomes from 3-methylcholanthrene-treated rats, two major hydroxylated metabolites were identified. Using inhibitory antibodies specific for individual cytochrome P-450 isozymes, cytochromes P-450 1A1, 1A2, and 3A were identified to be involved in dantrolene hydroxylations. In liver microsomes from 3-methylcholanthrene-treated rats, antibodies specific for cytochrome P-450 1A1 and 1A2 inhibited hydroxylation of dantrolene by 60% and 20%, respectively. Kinetics studies using these microsomes showed that dantrolene hydroxylation was biphasic with a low KM (0.06-0.08 microM) and high KM (5-7 microM). Cytochrome P-450 1A1 was responsible for the low KM hydroxylation of dantrolene, whereas cytochrome P-450 1A2 was responsible for the high KM. In hepatic microsomes from pregnenolone-16 alpha-carbonitrile-treated rats, an antibody specific for cytochrome P-450 3A completely inhibited the formation of 5-hydroxydantrolene, the major metabolite formed by these microsomes.

 

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Drug Metabolism and Disposition
Vol. 21, Issue 5
1 Sep 1993
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Abstract

Identification of cytochrome P-450 isozymes involved in the hydroxylation of dantrolene by rat liver microsomes.

Z Jayyosi, J Villoutreix, J M Ziegler, A M Batt, F De Maack, G Siest and P E Thomas
Drug Metabolism and Disposition September 1, 1993, 21 (5) 939-945;

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Abstract

Identification of cytochrome P-450 isozymes involved in the hydroxylation of dantrolene by rat liver microsomes.

Z Jayyosi, J Villoutreix, J M Ziegler, A M Batt, F De Maack, G Siest and P E Thomas
Drug Metabolism and Disposition September 1, 1993, 21 (5) 939-945;
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