Pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-deoxy-2',3'-didehydrothymidine in rats
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چکیده
منابع مشابه
Comparisons of anti-human immunodeficiency virus activities, cellular transport, and plasma and intracellular pharmacokinetics of 3'-fluoro-3'-deoxythymidine and 3'-azido-3'-deoxythymidine.
3'-Fluoro-3'-deoxythymidine (FLT), a candidate anti-AIDS compound in clinical trials, showed anti-human immunodeficiency virus type 1 (HIV-1) potency (50% effective concentration, 0.0052 microM) slightly better than or equal to that of 3'-azido-3'-deoxythymidine (AZT) in MT4 cells and was threefold more potent in H9 cells. There was no FLT resistance demonstrable in the AZT-resistant HIV-1 stra...
متن کاملIn vitro and in vivo disposition and metabolism of 3'-deoxy-2',3'-didehydrothymidine.
The disposition and metabolic fate of 3'-deoxy-2',3'-didehydrothymidine (D4T) were evaluated both in isolated hepatocytes and in nonhuman primates. Rapid formation of thymine and beta-aminoisobutyric acid (BAIBA) occurred following incubation of hepatocytes with 10 microM [5(-3)H]D4T. Substantial levels of tritiated water were also detected. Exposure of cells to D4T in the presence of either 1 ...
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Development of the positron emission tomography (PET) diagnostic radiopharmaceutical (18F) fluoro-2-deoxy-D-glucose (18F-FDG) subsequently facilitated the discovery and clinical evaluation of several new tracers as imaging markers for cancer. While 18F-FDG is a widely employed marker for enhanced intracellular glycolysis and metabolic function, one of the newer tracers, (18F)-3’-fluoro-3’ deoxy...
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Our objective was to determine whether age effects the pharmacokinetics of stavudine (2',3'-didehydro-3'-deoxythymidine) in the neonatal pig-tailed macaque (Macaca nemestrina). The drug (5 mg/kg of body weight) was administered serially as a single intravenous bolus to the same four macaques at the ages of < 1 week, 1 month, and 4 months. Plasma clearance at < 1 week of age was significantly lo...
متن کامل3'-Fluoro-3'-deoxy-5'-noraristeromycin derivatives: synthesis and antiviral analysis.
The promising antiviral properties of 3'-fluoro-3'-deoxyadenosine and 4',4'-difluoro-4'-deoxy-5'-noraristeromycin prompted the synthesis of the corresponding 3'-fluoro derivatives of 5'-noraristeromycin. These target compounds, which were prepared from the same readily accessible cyclopentenol, were found to be inactive when subjected to 31 viral assays. The results have some implications on th...
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 1991
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.35.4.747