Analysis of 2-(3-methyl-4-aminophenyl)-benzothiazole (NSC 674495) in plasma by gas chromatography with mass-selective detection
| Autor: | John Buckley, Tracy W. Daw, Sherman F. Stinson, Lawrence R. Phillips, Chris Bramhall |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Quality Control
Metabolite Antineoplastic Agents Sensitivity and Specificity Gas Chromatography-Mass Spectrometry chemistry.chemical_compound In vivo Blood plasma Animals Humans Benzothiazoles Aniline Compounds Chromatography biology Reproducibility of Results General Chemistry In vitro Rats Thiazoles Benzothiazole chemistry Enzyme inhibitor Calibration biology.protein Gas chromatography Quantitative analysis (chemistry) |
| Zdroj: | Journal of Chromatography B: Biomedical Sciences and Applications. 732:315-321 |
| ISSN: | 0378-4347 |
| DOI: | 10.1016/s0378-4347(99)00295-9 |
| Popis: | Certain naturally occurring isoflavonoids have been shown to inhibit protein-tyrosine kinases, and this has led to investigations of ring-modified structural analogs. Most recently, 2-(3-methyl-4-aminophenyl)-benzothiazole (MAB: NSC 674495) was shown to possess significant activity against certain breast cell cancer lines in vitro and in vivo. Our efforts thus focussed on developing a simple and sensitive method for quantitating MAB in plasma using GC-MS. The GC-MS assay was found to be linear over the range of 0.050 to 5.0 microg/ml, and was applied to monitor the plasma concentration of MAB in a rat dosed with 25 mg/kg as a 1 min intravenous infusion. Plasma was collected at intervals from 3 through 180 min, and concentrations of MAB were determined. Non-linear regression analysis of the plasma concentration-time data revealed that levels declined from a maximum at 3 min of 18 microg/ml to 1 microg/ml at 3 h in a biphasic manner. In another investigation, significant plasma concentrations of a major metabolite was detected and determined to be mono-N-acetylated MAB. |
| Databáze: | OpenAIRE |
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