Abstract
Oseltamivir phosphate (Tamiflu, 1.H(3)PO(4) is an orally active anti-influenza drug, which is hydrolyzed by esterase to its carboxylate metabolite Ro 64-0802 (2) with potent activity inhibiting neuraminidase. In this study, for the first time, we synthesized carbon-11-labeled oseltamivir ([(11)C]1) and Ro 64-0802 ([(11)C]2) as two novel positron emission tomography probes and demonstrated that [(11)C]1 had twofold higher radioactivity concentration in the mouse brains than [(11)C]2.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetamides / blood
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Acetamides / chemical synthesis*
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Acetamides / pharmacokinetics
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Animals
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Brain / diagnostic imaging
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Brain / metabolism
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Carbon Radioisotopes / blood
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Carbon Radioisotopes / chemistry*
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Isotope Labeling / methods
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Mice
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Oseltamivir / blood
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Oseltamivir / chemical synthesis*
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Oseltamivir / pharmacokinetics
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Positron-Emission Tomography / methods
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics
Substances
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Acetamides
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Carbon Radioisotopes
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Radiopharmaceuticals
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Ro 64-0802
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Oseltamivir