Disposition of allylic oxidation pathway metabolites of racemic hexobarbital in the rat

European Journal of Drug Metabolism and Pharmacokinetics
M Van der GraaffD D Breimer

Abstract

The pharmacokinetics in blood of the major metabolites of hexobarbital (HB), 3'-hydroxyhexobarbital (OH-HB) and 3'-ketohexobarbital (K-HB) were studied in rats. In addition urinary excretion of OH-HB and K-HB and 1,5-dimethylbarbituric acid (DMBA) was determined. Half-lives of OH-HB and K-HB were slightly longer than that of the parent drug. Urinary recovery of OH-HB, K-HB and DMBA following i.a. administration of OH-HB (75%) was more complete than the recovery following i.a. administration of K-HB (52%). Most probably further metabolism of K-HB takes place. Of K-HB, 41% was excreted renally, and 3.4% of K-HB reverted back to OH-HB. Of OH-HB, about 45% was excreted renally, following p.o. or i.a. administration. Since about 10% of both OH-HB and K-HB was converted to DMBA, it seems that the epoxide-diol pathway as proposed for HB also plays a minor role in the metabolism of OH-HB and K-HB. It is further concluded that measuring allylic pathway oxidation metabolites of HB does not improve the usefulness of HB as a model compound in the assessment of the activity of oxidative drug metabolizing activity.

References

Jun 1, 1977·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·R Takenoshita, S Toki
May 1, 1979·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·N P VermeulenD D Breimer
Jan 1, 1978·Biochemical Pharmacology·N P VermeulenA van der Gen
Jul 1, 1983·Toxicology and Applied Pharmacology·M E GrosmanE A Rodriguez Garay
Apr 1, 1983·British Journal of Clinical Pharmacology·N P VermeulenD D Breimer

❮ Previous
Next ❯

Citations

Jan 1, 1988·Drug Metabolism Reviews·M van der GraaffD D Breimer
Aug 1, 1993·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·R TakenoshitaS Toki
Nov 10, 2005·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·U YasarA Al-Shurbaji

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Drug Metabolism and Disposition : the Biological Fate of Chemicals
M Van der GraaffD D Breimer
The Journal of Pharmacology and Experimental Therapeutics
M Van der GraaffD D Breimer
Xenobiotica; the Fate of Foreign Compounds in Biological Systems
N P VermeulenA van der Gen
© 2021 Meta ULC. All rights reserved