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N‐Demethylation of Aminopyrine by the Nasal Mucosa in Mice and Rats

N‐Demethylation of Aminopyrine by the Nasal Mucosa in Mice and Rats Abstract: N‐demethylation of aminopyrine was demonstrated in the nasal mucosa of C57 B1 mice and Sprague‐Dawley rats by measurements of the 14CO2 formed at incubation of 14C‐aminopyrine with tissue‐slices. The metabolism of aminopyrine by the nasal mucosa was induced by phenobarbital pretreatment and susceptible to inhibition with metyrapone and SKF 525 A suggesting the presence of a cytochrome P‐450‐dependent enzyme system in the tissue. Immediately after injection of 14C‐aminopyrine in rats a uniform distribution of radioactivity in the body was recorded. After thirty minutes, however, a preferential localization of radioactivity was found in the nasal mucosa and in the liver. By pretreatment with metyrapone the uptake of radioactivity in the nasal mucosa and in the liver was blocked suggesting that the observed accumulation of radioactivity is due to metabolites. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Basic and Clinical Pharmacology & Toxicology Wiley

N‐Demethylation of Aminopyrine by the Nasal Mucosa in Mice and Rats

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References (20)

Publisher
Wiley
Copyright
Copyright © 1982 Wiley Subscription Services, Inc., A Wiley Company
ISSN
1742-7835
eISSN
1742-7843
DOI
10.1111/j.1600-0773.1982.tb01018.x
Publisher site
See Article on Publisher Site

Abstract

Abstract: N‐demethylation of aminopyrine was demonstrated in the nasal mucosa of C57 B1 mice and Sprague‐Dawley rats by measurements of the 14CO2 formed at incubation of 14C‐aminopyrine with tissue‐slices. The metabolism of aminopyrine by the nasal mucosa was induced by phenobarbital pretreatment and susceptible to inhibition with metyrapone and SKF 525 A suggesting the presence of a cytochrome P‐450‐dependent enzyme system in the tissue. Immediately after injection of 14C‐aminopyrine in rats a uniform distribution of radioactivity in the body was recorded. After thirty minutes, however, a preferential localization of radioactivity was found in the nasal mucosa and in the liver. By pretreatment with metyrapone the uptake of radioactivity in the nasal mucosa and in the liver was blocked suggesting that the observed accumulation of radioactivity is due to metabolites.

Journal

Basic and Clinical Pharmacology & ToxicologyWiley

Published: Sep 1, 1982

Keywords: ; ; ; ;

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