title: Radiosyntheses of two positron emission tomography probes: [11C]Oseltamivir and its active metabolite [11C]Ro 64-0802.
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.
authors.affiliation: Radiochemistry Section, Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
authors.forename: Fujiko
authors.initials: F
authors.lastname: Konno
authors.forename: Takuya
authors.initials: T
authors.lastname: Arai
authors.forename: Ming-Rong
authors.initials: MR
authors.lastname: Zhang
authors.forename: Akiko
authors.initials: A
authors.lastname: Hatori
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Yanamoto
authors.forename: Masanao
authors.initials: M
authors.lastname: Ogawa
authors.forename: Gukuto
authors.initials: G
authors.lastname: Ito
authors.forename: Chika
authors.initials: C
authors.lastname: Odawara
authors.forename: Tomoteru
authors.initials: T
authors.lastname: Yamasaki
authors.forename: Koichi
authors.initials: K
authors.lastname: Kato
authors.forename: Kazutoshi
authors.initials: K
authors.lastname: Suzuki
mesh_terms: D000081:Acetamides / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000097:blood / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D051379:Mice; D053139:Oseltamivir / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics
chemical_list: D000081:Acetamides; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; C403132:Ro 64-0802; D053139:Oseltamivir