Related Experiment Video
Updated: Aug 13, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
Biotransformation and excretion of nitromethaqualone in rats and humans
Abstract:
The metabolic disposition of 14C-labeled nitromethaqualone was investigated in rats. Unlabeled nitromethaqualone was used for studies on humans. nitromethaqualone was eliminated from the body after most of it had undergone biotransformation. Both humans and rats reduced the nitro group of nitromethaqualone to the corresponding amino derivative, which was partially transformed to the corresponding acetylated form. Cleavage of the quinazolinone nucleus resulting in 2-methoxyl-4-nitroaniline was also observed in humans. In rats additional major metabolites arose from the oxidation of the 2-methyl group into hydroxymethyl resulting in 2-hydroxymethyl-3-(2'-methoxy-4-nitrophenyl)-4(3H)-quinazolinone and concomitant in vivo reduction of the latter resulting in 2-hydroxymethyl-3-(2'-methoxy-4'-aminophenyl)-4(3H)-quinazolinone. Both metabolites were also excreted as glucuronides. In rats fecal excretion accounted for 55-60% of the administered dose, while 24-27% was excreted in the urine. Protracted excretion in both humans and rats indicated an extensive enterohepatic circulation.
More Related Videos
07:38A General Method for Detecting Nitrosamide Formation in the In Vitro Metabolism of Nitrosamines by Cytochrome P450s
Published on: September 25, 2017
08:28Microsurgical Skills of Establishing Permanent Jugular Vein Cannulation in Rats for Serial Blood Sampling of Orally Administered Drug
Published on: December 14, 2021
Related Concept Videos
Drug Biotransformation: Overview
Drug Elimination: Non-Renal Routes
Drug Biotransformation: Overview
Drug Elimination: Overview
Excretion refers to removing a drug from the body, either in its unchanged form or as its metabolites. Nonvolatile and polar drugs are primarily excreted through the kidneys, with other pathways including bile, sweat, saliva, and milk. Volatile drugs such as anesthetic gases are excreted via the...
Drug Excretion: Miscellaneous Routes
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase