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Acute toxicity and effects on hepatic oxidative drug metabolism of mopyridone.

Abstract
Mopyridone (CAS 82822-14-8) is a new chemotherapeutic with a strong antiviral effect (vs. influenza- and toga viruses) and certain advantages over the chemotherapeutics known so far. Toxicological studies reveal its low oral and intraperitoneal toxicity in mice and rats. The 5- and 14-day administration of mopyridone (37.5 mg/kg b.w., orally) to male rats established a growing tendency to the shortening of hexobarbital sleeping time, associated with moderate changes in the hepatic oxidase activity on the 15th day, most pronounced for amidopyrine N-demethylase (by 37%) and less for benzphetamine N-demethylase (by 17%). Aniline hydroxylase activity was slightly diminished (by 18% and 16%, resp.). No significant changes in the components of the electron-transport chain of cytochrome P-450 were established--the content of cytochrome P-450, cytochrome b-5 and cytochrome C reductase, both after 5- and 14-day mopyridone administration.
AuthorsL Tantcheva, A S Galabov, M Behar, D Sidzhakova
JournalArzneimittel-Forschung (Arzneimittelforschung) Vol. 44 Issue 3 Pg. 354-7 (Mar 1994) ISSN: 0004-4172 [Print] Germany
PMID8192702 (Publication Type: Journal Article)
Chemical References
  • Antiviral Agents
  • Pharmaceutical Preparations
  • Pyrimidinones
  • Hexobarbital
  • 1-morpholinomethyl-tetrahydro-1(1H)-pyrimidinone
  • Mixed Function Oxygenases
Topics
  • Animals
  • Antiviral Agents (pharmacology, toxicity)
  • Female
  • Hexobarbital (pharmacology)
  • Lethal Dose 50
  • Liver (drug effects, enzymology, metabolism)
  • Male
  • Mice
  • Microsomes, Liver (drug effects, enzymology)
  • Mixed Function Oxygenases (metabolism)
  • Oxidation-Reduction
  • Pharmaceutical Preparations (metabolism)
  • Pyrimidinones (pharmacology, toxicity)
  • Rats
  • Rats, Wistar
  • Sleep (drug effects)

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