APPLICATION OF CHEMICAL P-450 MODEL SYSTEMS TO STUDY DRUG-METABOLISM .3. METABOLISM OF 3-ISOBUTYRYL-2-ISOPROPYLPYRAZOLO[1,5-A]PYRIDINE

被引:22
作者
NAGATSU, Y [1 ]
HIGUCHI, T [1 ]
HIROBE, M [1 ]
机构
[1] UNIV TOKYO, FAC PHARMACEUT SCI, BUNKYO KU, TOKYO 113, JAPAN
关键词
5-a]pyridine: metabolism: liver microsome- oxidation P-450 chemical model P-450 mimic metalloporphyrin; anti-asthma cerebral vasodilator: 3-isobutyryl-2-isopropylpyrazolo[1;
D O I
10.1248/cpb.38.400
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Oxidation of 3-isobutyryl-2-isopropylpyrazolo[l,5-a]pyridine (IBPP) was carried out with various chemical model systems for cytochrome P-450 in comparison with the liver microsomal system of rats or humans. a-Hydroxylation of side chains and ring hydroxylation at the 6 and 7 positions were the main reactions in both systems. A pattern analysis of products using two dimensional thin layer chromatography was employed to compare the functions of the chemical model systems with those of microsomal systems. The reaction profile of IBPP by the catalyst/Pt-colloid/H2, 02 system was most similar to that of human or rat microsomal system. The utility of these chemical models is discussed from the viewpoint of drug metabolism. © 1990, The Pharmaceutical Society of Japan. All rights reserved.
引用
收藏
页码:400 / 403
页数:4
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