While assessing the ability of mammalian lung tissue to metabolize theophylline, a new metabolite was isolated and characterized. The metabolite was produced by the microsomal fraction of lungs from several species, including rat, rabbit, dog, pig, sheep and human tissue. Metabolite production was blocked by boiling the microsomal tissue. This new metabolite, theophylline-7β-d-ribofuranoside (t...

Mechanism-based inhibition of CYP2B6 in human liver microsomes by thienopyridine antiplatelet agents ticlopidine and clopidogrel and the thiolactone metabolites of those two agents plus that of prasugrel were investigated by determining the time- and concentration-dependent inhibition of the activity of bupropion hydroxylase as the typical CYP2B6 activity. By comparing the ratios of k(inact) (m...

The structure of a major active metabolite of the nonsedating antihistamine loratadine was confirmed by synthesis. The metabolite 3 was prepared from 3-methyl pyridine in twelve steps.

OBJECTIVE Proton magnetic resonance spectroscopy (1H MRS) in opiate dependence showed abnormalities in neuronal viability and glutamate concentration in the anterior cingulate cortex (ACC). Metabolite levels in dorsolateral prefrontal cortex (DLPFC) or orbitofrontal cortex (OFC) and their neuropsychological correlates have not been investigated in opiate dependence. METHODS Single-volume prot...

SUMMARY Proton MR spectroscopy is a powerful noninvasive method that enables measurement of certain brain metabolites in healthy subjects and patients with diseases. A major difficulty with clinical and research applications of in vivo proton MR spectroscopy is the variability of metabolite concentrations, especially in regions with substantial physiologic motion. In our preliminary evaluation,...

Vabicaserin is a potent 5-hydroxtryptamine 2C full agonist with therapeutic potential for a wide array of psychiatric disorders. Metabolite profiles indicated that vabicaserin was extensively metabolized via carbamoyl glucuronidation after oral administration in humans. In the present study, the differences in the extent of vabicaserin carbamoyl glucuronide (CG) formation in humans and in anima...

To improve reproducibility in proton magnetic resonance (MR) spectroscopic imaging in human brain, simultaneous acquisition of the internal water reference and metabolite signals was evaluated. Measurements in healthy volunteers showed that the increase in dynamic range from signal oversampling was sufficient to avoid digitization errors. In addition, use of singular value decomposition techniq...

Several metabolites of tamoxifen, including 4-hydroxy-N-desmethyltamoxifen (metabolite BX), 4-hydroxytamoxifen (metabolite B), N-desmethyltamoxifen (metabolite X), the primary alcohol (metabolite Y), and N-desdimethyltamoxifen (metabolite Z) were identified and their concentrations determined in fluids and feces from patients receiving chronic tamoxifen treatment. The biological samples investi...

Metabolite in safety testing has been proposed for toxicity assessments. The question of how exposure of the synthetic metabolite compared with that of the formed metabolite was appraised kinetically by using physiologically based pharmacokinetic models, the (traditional) physiological model (TM), and segregated flow (SFM) models. The SFM differs from the TM and describes a partial (approximate...

Metabolite-content (MC) refers to all small molecules which are the products or intermediates of metabolism within an organism. The metabolite-contents of plants which involve numerous secondary metabolites are highly related to their nutritional and medicinal features. Previous researches have confirmed that phylogeny-guided approaches have been seen as one of the timeefficient and informative...