[原著］ENHANCEMENT OF HEPATIC MICROSOMALAMINO・PYRINE N-DEMETHYLATION BY NEUTRAL SALTS
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Enhancement of aminopyrine N-demethylation by neutral salts was kinetically studied using hepatic microsomes from nontreated, phenobarbital- or 3-methylcholanthrene-treated rats. Aminopyrine N-demethylation was increased 3-fold by 0.4 M sodium sulfate in nontreated or 3-methylcholanthrene-treated microsomes. On the other hand, the enhancement was 1.7-fold in phenobarbital-treated microsomes. Lineweaver-Burk plots of aminopyrine N-demethylase were not linear in nontreated microsomes and two Km values (2X10^<-3>M, 5X10^<-4>M) were obtained. However, the addition of neutral salts to the microsomes brought on a linear Lineweaver-Burk plots of the demethylation and only one km, which was less than 2X10^<-3>M. Aminopyrine-induced difference spectra of the microsomes were increased by the addition of neutral salts, and double reciprocal plots of the spectrum vs aminopyrine concentration were linear, though the plots were not linear in absence of the salts. Dissociation constant (Ks) values were also decreased by the addition of neutral salts corresponding enhancement of the demethylation, as were the km values. In phenobarbital or 3-methylcholanthrene-treated microsomes one Km was obtained regardless of the presence or absence of sodium sulfate, though Km of the demethylase in the former microsomes was higher than that in the latter after addition of the salt. These results suggest that there are multiple forms of aminopyrine N-demethylase in nontreated and 3-methylcholanthrene -treated microsomes and some of them slightly contribute to the demethylation in normal condition but exhibite the demethylase activity by addition of the salts. Phenobarbital may induce the aminopyrine N-demethylase capable of demethylating aminopyrine in normal condition resulted in less enhancement of the demethylation by the salts.
- 琉球大学医学部の論文
- 1986-00-00
琉球大学医学部 | 論文
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