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Chemical Compound Review:

AG-J-24754 5-ethyl-5-(4-hydroxyphenyl)- 1,3-diazinane...

Synonyms: CHEMBL1908024, NSC-159266, AC1L1TTD, AC1Q6GBZ, CTK4H9034, ...

Cresteil, T. et al., Xiong, H. et al., Riva, R. et al., Levin, S.S. et al., Patel, I.H. et al., et al.

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Disease relevance of NSC 159266

In animals with bile fistulas most of the 14C-phenobarbital was excreted in bile as p-hydroxyphenobarbital conjugated with glucuronic acid [1].

High impact information on NSC 159266

The pharmacokinetics and pharmacodynamics of p-hydroxyphenobarbital, the main metabolite of phenobarbital, also were investigated [2].
However, AG significantly inhibited Mrp2-mediated 5-(and 6)-carboxy-2',7'-dichlorofluorescein (CDF) transport. p-Hydroxyphenobarbital glucuronide (p-OHPBG), but not PB or p-hydroxyphenobarbital, significantly inhibited Mrp2-mediated CDF transport [3].
GC and GC-mass spectrometric determination of p-hydroxyphenobarbital extracted from plasma, urine, and hepatic microsomes [4].
Simultaneous analysis of phenobarbital and p-hydroxyphenobarbital in biological fluids by GLC-chemical-ionization mass spectrometry [5].
Rapid quantitative determination of underivatized carbamazepine, phenytoin, phenobarbital and p-hydroxyphenobarbital in biological fluids by packed column gas chromatography [6].

Biological context of NSC 159266

The elimination rate of p-hydroxyphenobarbital was constant, suggesting capacity limited kinetics [7].
In five-day-old newborns, p-hydroxyphenobarbital provoked a proliferation of endoplasmic reticulum without enzyme induction, whereas phenobarbital induced some drug-metabolizing enzymes [8].

Anatomical context of NSC 159266

Thus, the effects of p-hydroxyphenobarbital and phenobarbital are retained in five-day-old rats, but undetectable in the fetuses [8].

Gene context of NSC 159266

Drug-metabolizing enzymes (cytochrome P450, epoxide hydrolase, UDP-glucuronosyltransferase, and glutathione-S-transferase) and microsomal ribonuclease were not modified in fetuses treated with 80 or 400 mg . kg-1 of p-hydroxyphenobarbital, in spite of its accumulation in fetal liver [8].

Analytical, diagnostic and therapeutic context of NSC 159266

PB and p-hydroxyphenobarbital (p-OHPB) in serum and urine were measured by high-performance liquid chromatography (HPLC) [9].
However, the percentage of conjugated p-hydroxyphenobarbital excreted, was almost twice that of the control group [10].

References

The metabolism and excretion of enzyme-inducing doses of phenobarbital by rats with bile fistulas. Levin, S.S., Vars, H.M., Schleyer, H., Cooper, D.Y. Xenobiotica (1986) [Pubmed]
Pharmacokinetic modeling of the anticonvulsant action of phenobarbital in rats. Dingemanse, J., van Bree, J.B., Danhof, M. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
Mechanisms of impaired biliary excretion of acetaminophen glucuronide after acute phenobarbital treatment or phenobarbital pretreatment. Xiong, H., Suzuki, H., Sugiyama, Y., Meier, P.J., Pollack, G.M., Brouwer, K.L. Drug Metab. Dispos. (2002) [Pubmed]
GC and GC-mass spectrometric determination of p-hydroxyphenobarbital extracted from plasma, urine, and hepatic microsomes. Kapetanović, I.M., Kupferberg, H.J. Journal of pharmaceutical sciences. (1981) [Pubmed]
Simultaneous analysis of phenobarbital and p-hydroxyphenobarbital in biological fluids by GLC-chemical-ionization mass spectrometry. Patel, I.H., Levy, R.H., Neal, J.M., Trager, W.F. Journal of pharmaceutical sciences. (1980) [Pubmed]
Rapid quantitative determination of underivatized carbamazepine, phenytoin, phenobarbital and p-hydroxyphenobarbital in biological fluids by packed column gas chromatography. Riva, R., Albani, F., Baruzzi, A. J. Chromatogr. (1980) [Pubmed]
Phenobarbital disposition in the neonate. Garrettson, L.K. Addictive diseases. (1975) [Pubmed]
Comparison of the effects of phenobarbital and its hydroxylated metabolites on drug-metabolizing enzymes during ontogenesis. Cresteil, T., Mahu, J.L., Beaune, P., Columelli, S., Leroux, J.P. Pediatric pharmacology (New York, N.Y.) (1981) [Pubmed]
P-hydroxylation of phenobarbital: relationship to (S)-mephenytoin hydroxylation (CYP2C19) polymorphism. Hadama, A., Ieiri, I., Morita, T., Kimura, M., Urae, A., Irie, S., Kaneda, T., Mamiya, K., Tashiro, N., Higuchi, S., Otsubo, K. Therapeutic drug monitoring. (2001) [Pubmed]
Effect of diphenylhydantoin and its main hydroxylated metabolite on the pharmacokinetics and the urinary and biliary excretion of phenobarbital and its p-hydroxy metabolite. Sarhan, F., Engasser, J.M., Batt, A.M., Magdalou, J., Siest, G. European journal of drug metabolism and pharmacokinetics. (1981) [Pubmed]

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