4,4'-DIHYDROXYPHENAZONE AS AN URINARY METABOLITE OF PHENAZONE IN DIFFERENT SPECIES INCLUDING MAN

被引:26
作者
BASSMANN, H [1 ]
BOTTCHER, J [1 ]
SCHUPPEL, R [1 ]
机构
[1] TECH UNIV BRUNSWICK,INST PHARMAKOL & TOXIKOL,D-3300 BRUNSWICK,FED REP GER
关键词
Biotransformation; Drug hydroxylation; Phenazone/antipyrine; Secondary metabolites;
D O I
10.1007/BF00501230
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
4,4′-Dihydroxyphenazone (4-hydroxy-1-(4′-hydroxyphenyl)-2,3-dimethyl-3-pyrazoline-5-one) was isolated as a metabolite of phenazone (antipyrine) after acid hydrolysis of rat urine. This was characterized and identified by NMR, MS, IR, UV, Fp and ε270. After dosage with phenazone, 4,4′-dihydroxyphenazone is excreted in conjugated form by man, rabbit, guinea pig and rat. In the rat it is further shown, that conjugates of 4,4′-dihydroxyphenazone are formed by glucuronidation as well as by sulfatation. The metabolite seems to add substantially to the overall metabolic pattern of phenazone in these species. © 1979 Springer-Verlag.
引用
收藏
页码:203 / 205
页数:3
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