Excretion of 4-formylaminoantipyrine as a new metabolite of aminopyrine in experimental animals.

After i.p. injection of 3-14C-antipyrine (10 micronmole = 1.9 mg with 10 micronCi per 10 g of body weight) to mice radioactivity was irreversibly bound to liver proteins. The irreversible binding reached maximal values of 0.15 nmole/mg protein in liver microsomes after 30-60 min. During 60 min incubation with liver microsomes of mice and rabbits (phenobarbital pretreated) and a NAKPH-regenerating system 3-14C-antipyrine was irreversibly bound to microsomal protein at a rate of 1.5 nmole/mg protein (mouse) and 3 nmole/mg protein (rabbit). In identical incubates with rabbit liver microsomes the 4-hydroxylation of antipyrine was 24 nmole/mg protein in 60 min and formaldehyde production from antipyrine 3 nmole/mg protein in 60 min. In incubates with rabbit liver microsomes the binding rate was 80-90% inhibited by 1mM metyrapone, SKF 525-A and trichloropropene epoxide respectively; 4-hydroxylation was 70-80% inhibited by the same substances. In the presence of 1mM GSH, cysteine or ethylene diamine binding was 30-40% inhibited, whereas 4-hydroxylation showed no inhibition.

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Irreversible binding of 3-14C-antipyrine to hepatic protein in vivo and in metabolizing liver microsomes

Tabarelli-Poplawski

Uehleke

1977

Naunyn-Schmiedeberg's Arch. Pharmacol.

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Simple high-performance liquid chromatographic method for simultaneous determination of aminopyrine and its metabolites

D’Souza

Zemaitis

Burckart

et al. 1987

Journal of Chromatography B: Biomedical Sciences and Applicatio

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Histological studies into rat liver following long-term application of aminophenazone, phenazone, and propyphenazone

Buntrock

Bien

Neubauer

1986

Experimental pathology

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Excretion of 4-formylaminoantipyrine as a new metabolite of aminopyrine in experimental animals.

Cited by 8 publications

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Irreversible binding of 3-14C-antipyrine to hepatic protein in vivo and in metabolizing liver microsomes

Irreversible binding of 3-14C-antipyrine to hepatic protein in vivo and in metabolizing liver microsomes

Simple high-performance liquid chromatographic method for simultaneous determination of aminopyrine and its metabolites

Histological studies into rat liver following long-term application of aminophenazone, phenazone, and propyphenazone

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