Literature DB >> 1726081

Aminopyrine-N-demethylase. I. Directed modification of substrates' structure as a way of production of inducer of the monooxygenase isoform P-450b.

I B Tsyrlov1, K E Gerasimov.   

Abstract

The effect of the phenobarbital-type monooxygenase inducers is accomplished via the native molecule. This made it possible to transform the typical substrate of cytochrome P-450b aminopyrine into an inducer of this isozyme by blocking the substrate molecule position undergoing monooxygenation. Substitution of two methyl groups in the aminopyrine -N(CH3)2 position by an isopropyl group gave rise to a clear-cut inducive effect. This was registered by spectral, kinetic, radiological and immunochemical methods.

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Year:  1991        PMID: 1726081     DOI: 10.1007/BF03189961

Source DB:  PubMed          Journal:  Eur J Drug Metab Pharmacokinet        ISSN: 0378-7966            Impact factor:   2.441


  15 in total

1.  The fate of aminopyrine (pyramidon) in man and methods for the estimation of aminopyrine and its metabolites in biological material.

Authors:  B B BRODIE; J AXELROD
Journal:  J Pharmacol Exp Ther       Date:  1950-06       Impact factor: 4.030

2.  Structure-activity relationships in polycyclic aromatic hydrocarbons: induction of microsomal aryl hydrocarbon hydroxylase and its possible importance in chemical carcinogenesis.

Authors:  R Franke
Journal:  Chem Biol Interact       Date:  1973-01       Impact factor: 5.192

3.  Cleavage of structural proteins during the assembly of the head of bacteriophage T4.

Authors:  U K Laemmli
Journal:  Nature       Date:  1970-08-15       Impact factor: 49.962

4.  Fluorographic detection of radioactivity in polyacrylamide gels with the water-soluble fluor, sodium salicylate.

Authors:  J P Chamberlain
Journal:  Anal Biochem       Date:  1979-09-15       Impact factor: 3.365

5.  Possible mechanism of induction of liver microsomal monooxygenases by phenobarbital.

Authors:  I B Tsyrlov; N E Zakharova; O A Gromova; V V Lyakhovich
Journal:  Biochim Biophys Acta       Date:  1976-01-14

6.  In vivo administration of hydroxylated phenobarbital metabolites: effect on rat hepatic cytochromes P-450, epoxide hydrolase and UDP-glucuronosyltransferase.

Authors:  T Cresteil; J L Mahu; P M Dansette; J P Leroux
Journal:  Biochem Pharmacol       Date:  1980-04-15       Impact factor: 5.858

7.  Separation of pure polychlorinated biphenyl isomers into two types of inducers on the basis of induction of cytochrome P-450 or P-448.

Authors:  J A Goldstein; P Hickman; H Bergman; J D McKinney; M P Walker
Journal:  Chem Biol Interact       Date:  1977-04       Impact factor: 5.192

8.  Studies of the metabolism of diethyl p-nitrophenyl phosphorothionate (parathion) and benzphetamine using an apparently homogeneous preparation of rat liver cytochrome P-450: effect of a cytochrome P-450 antibody preparation.

Authors:  T Kamataki; D H Belcher; R A Neal
Journal:  Mol Pharmacol       Date:  1976-11       Impact factor: 4.436

9.  [Correlation between cytochrome P-448 content and benzopyrene hydroxylase activity during the induction of microsomal monooxygenases using methylcholanthrene-type xenobiotics].

Authors:  V M Mishin; S I Makarova; N I Gutkina; A Iu Grishanova; V V Liakhovich
Journal:  Biokhimiia       Date:  1984-03

10.  Structure-activity relationships in halogenated biphenyls: unifying hypothesis for structural specificity.

Authors:  J D McKinney; P Singh
Journal:  Chem Biol Interact       Date:  1981-01       Impact factor: 5.192

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  1 in total

1.  Aminopyrine-N-demethylase. II. Characterization of a unique monooxygenase isoform P-450ap.

Authors:  I B Tsyrlov; K E Gerasimov
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1991 Jul-Sep       Impact factor: 2.441

  1 in total

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