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  • Title: Radiosyntheses of two positron emission tomography probes: [11C]Oseltamivir and its active metabolite [11C]Ro 64-0802.
    Author: Konno F, Arai T, Zhang MR, Hatori A, Yanamoto K, Ogawa M, Ito G, Odawara C, Yamasaki T, Kato K, Suzuki K.
    Journal: Bioorg Med Chem Lett; 2008 Feb 15; 18(4):1260-3. PubMed ID: 18226899.
    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.
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