N-Hydroxy-2-acetylaminofluorene (N-hydroxy-AAF), in conjugated form, was identified as a urinary metabolite of 2-acetylaminofluorene (AM') in male mongrel dogs. This metabolite was isolated and characterized in crystalline form. 7-Hydnoxy AM', in conjugated form, and AM? were also found in the urine of dogs fed AAF; no 1-, 3-, or 5-hydroxy-AAF was detected. The ingestion of N-hydroxy-AAF led to...

Therapeutic agents, in general, undergo chemical alteration in the body to form derivatives of the parent compound. Isolation and pharmacological assay of the various transformation products may yield valuable information in the Senrch for better therapeutic agents, in studies on the mechanism of drug action :,*d in the elucidation of norm+l metabolic processes. The therapeutic effect of a drug...

The effects of perazine on the activities of CYP1A2 and CYP3A4 in a primary culture of human hepatocytes of one patient were studied in vitro. The CYPs activities were assessed by measuring the rate of acetanilide 4-hydroxylation (CYP1A2) and cyclosporine A oxidation (CYP3A4) after treatment with TCDD (a CYP1A subfamily inducer) or rifampicin (mainly a CYP3A4 inducer). The amounts of the metabo...

Various aromatic molecules can behave as electron donors and form molecular complexes with electron acceptor molecules such as halogens, mitrocompounds and quinones. Extensive works have been carried out to elucidate the nature of intermolecular interactions in these molecular complexes. Mulliken has developed the theory of the intermolecular CT interactions, which has been applied successfully...