Proadifen

Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

The relationship between circadian rhythms in the pharmacological actions of meperidine and hexobarbital and similar rhythms in the hepatic metabolism of these drugs was examined in mice under a variety of environmental alterations to determine whether such rhythms may be causally related. The rate of metabolism of p-nitroanisole and hexobarbital by hepatic 9000 X g supernatant fractions was found to be higher at 2400 hours (middark phase) compared to 1200 hours (midlight phase).

Author(s): 
Holcslaw, T. L.
Miya, T. S.
Bousquet, W. S.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

The effect of methaqualone on the induction of hepatic enzymes was evaluated in rats and compared with that of phenobarbital by measuring effects on hexobarbital and methaqualone hypnosis, plasma and tissue levels of methaqualone, hepatic aniline hydroxylase and aminopyrine demethylase activity and warfarin-induced hypoprothrombinemia. Maximal reductions in hexobarbital hypnosis occurred 3 days after daily administration of 60 mg of methaqualone per kg per day.

Author(s): 
Mathur, P. P.
Smyth, R. D.
Herczeg, T.
Reavey-Cantwell, N. H.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Four pharmacologic actions of intravenous ketamine (30 mg/kg) were studied in the rat. To elucidate the mechanism(s) terminating the pharmacologic effects, animals were pretreated with ketamine and agents anticipated to modify hepatic microsomal metabolism, including phenobarbital and SKF 525A.

Author(s): 
Marietta, M. P.
White, P. F.
Pudwill, C. R.
Way, W. L.
Trevor, A. J.
Publication Title: 
Pharmacology
Author(s): 
Means, J. R.
Schnell, R. C.
Miya, T. S.
Bousquet, W. F.
Publication Title: 
Drug and Alcohol Dependence

Induction of hepatic propoxyphene N-demethylase and aniline hydroxylase activities resulted following repeated oral administration of 25, 50 and 100 mg d-propoxyphene hydrochloride per kg daily in the mouse over a six-day period. A significant elevation in both enzyme activities was noted after a single dose of propoxyphene (100 mg/kg). A dose-related response characterized the observed induction of each microsomal enzyme activity.

Author(s): 
Masten, L. W.
Publication Title: 
General Pharmacology

1. Pretreatment with a Cannabis constituent, cannabichromene (CBC), i.p., had no effect on in vitro hepatic microsomal enzyme activity compared to a known inhibitor of these systems, SKF 525-A. 2. The results indicate that the previously reported CBC potentiation of CNS depressant-induced hypnosis is not mediated by the hepatic microsomal enzyme system.

Author(s): 
Kapeghian, J. C.
Jones, A. B.
Murphy, J. C.
Elsohly, M. A.
Turner, C. E.
Publication Title: 
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica

The present study deals with the hypnotic effect of pentobarbital (Pento) in relation to its metabolism in hepatic microsomes in streptozotocin (STZ, 170 mg/kg, i.p.) injected mice. Liver weight (mg/10 g body wt.) of STZ-treated mice was larger than that of the controls throughout the experimental period. Although the shortening of sleeping time induced by Pento (60 mg/kg, i.p.) was always observed, Pento-metabolizing enzyme activity (by the method of Kato et al., 1964) increased in mice with diabetes for 2 and 4 weeks but decreased in mice with diabetes for 8 weeks.

Author(s): 
Fujii, E.
Tsukahara, F.
Nomoto, T.
Publication Title: 
Archives of Biochemistry and Biophysics

Metabolism of nitrosamines was studied in a reconstituted monooxygenase system composed of cytochrome P-450 isozymes purified from liver microsomes of ethanol- and phenobarbital-treated rats. The ethanol-induced isozyme (P-450et) was efficient in catalyzing the demethylation of N-nitrosodimethylamine (NDMA), with a Km of 2.4 mM and Vmax of 7.2 nmol min-1 nmol P-450(-1), but less active with N-nitrosomethylbenzylamine and N-nitrosomethylaniline.

Author(s): 
Tu, Y. Y.
Yang, C. S.
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