Journal ArticleDOI
Metabolism of Papaverine I. Identification of Metabolites in Rat Bile
Reads0
Chats0
TLDR
After hydrolysis with glusulase of bile from rats treated with papaverine, four metabolites (A, B, C and D) were separated and the structures A, B and C were established as monodemethylated compounds, 4'-desmethyl, 7-des methyl-, and 6-desmethylpapaverine.Abstract:
1. After hydrolysis with glusulase of bile from rats treated with papaverine, four metabolites (A, B, C and D) were separated.2. The structures of A, B and C were established as the monodemethylated compounds, 4′-desmethyl-, 7-desmethyl-, and 6-desmethylpapaverine, respectively.3. D was formed from papaverine by bis-demethylation. Since it was found in cat bile after administering either A or C, but not B, it was identified as 4′,6-desmethylpapaverine.read more
Citations
More filters
Book ChapterDOI
Microbial models for drug metabolism.
John P. Rosazza,Robert V. Smith +1 more
TL;DR: The routine screening of a carefully selected group of 10-40 microorganisms may be used to quickly assess the probability of producing drug metabolites, and the most striking similarities in microbial and mammalian metabolic systems lie in their respective cytochrome P450 hemoprotein monooxygenases.
Journal ArticleDOI
Changes in glutathione and cellular energy as potential mechanisms of papaverine-induced hepatotoxicity in vitro
TL;DR: It is suggested that the mechanism of papaver-induced hepatotoxicity may be related to alterations in glutathione balance of the cells and to disruption of energy homeostasis.
Journal ArticleDOI
Metabolism and metabolomics of opiates: A long way of forensic implications to unravel.
TL;DR: This work aims to review the metabolism and metabolomics of opiates with particular interest on their relevance as potential clinical and forensic antemortem and postmortem biomarkers of long-term heroin addiction.
Journal ArticleDOI
Assaying embryotoxicity in the test tube: Current limitations of the embryonic stem cell test (EST) challenging its applicability domain
Christian Riebeling,Katrin Hayess,Annelieke K. Peters,Margino Steemans,Horst Spielmann,Andreas Luch,Andrea Seiler +6 more
TL;DR: The EST performed well below the 78% accuracy expected from the validation study using a new set of chemicals and pharmaceutical compounds, and also of toxicity criteria, tested to enlarge the database of the validated EST.
Journal ArticleDOI
Microbial models of mammalian metabolism O-demethylations of papaverine.
John P. N. Rosazza,Marianne Kammer,Leisa Youel,Robert V. Smith,Paul W. Erhardt,Duyen H. Truong,Steven W. Leslie +6 more
TL;DR: The O-demethylation of papaverine was studied with sixty micro-organisms and ten organisms were found to actively metabolize this drug in a manner similar to that of mammals.
References
More filters
Journal Article
The fate of papaverine in man and other mammals.
Journal ArticleDOI
Metabolism of papaverine. II. Species differences.
Frans Belpaire,Marc G. Bogaert +1 more
TL;DR: The urinary and biliary excretion of radioactive products in a 6 hr period after intravenous administration of [3H]papaverine was studied in rat, guinea-pig, rabbit, cat and dog.
Journal ArticleDOI
Opium Alkaloids VII. Isolation of a New Benzylisoquinoline Alkaloid. Synthesis and NMR Studies of Papaveroline Trimethyl Ethers
TL;DR: A new phenolic alkaloid was isolated from opium and named palaudine and characterized spectroscopically as 1-(3′-hydroxy-4′-methoxybenzyl)-6,7-dimethoxyisoquinoline and the structure confirmed by synthesis.
Journal ArticleDOI
Metabolism of papaverine. III. Effect of phenobarbital, 3-methylcholanthrene and SKF 525-A pre-treated in vivo and in vitro.
Frans M. Belpaire,Bogaert Mg +1 more
TL;DR: Pre-treatment of rats with phenobarbital enhanced the activity of papaverine O-demethylase, whereas pre-treatment with 3-methylcholanthrene did not and pre- treatment with SKF 525-A markedly inhibited the enzyme.
Journal ArticleDOI
The excretion of 3H-papaverine in the rat
Frams M. Belpaire,Bogaert Mg +1 more
TL;DR: The results suggest that the bile is the main route of excretion of papaverine metabolites and that enterohepatic circulation of these metabolites is not important.
Related Papers (5)
Metabolism of papaverine. III. Effect of phenobarbital, 3-methylcholanthrene and SKF 525-A pre-treated in vivo and in vitro.
Frans M. Belpaire,Bogaert Mg +1 more