Radiosyntheses of two positron emission tomography probes: [11C]Oseltamivir and its active metabolite [11C]Ro 64-0802.
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.
Konno
Fujiko
F
Radiochemistry Section, Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
Arai
Takuya
T
Zhang
Ming-Rong
MR
Hatori
Akiko
A
Yanamoto
Kazuhiko
K
Ogawa
Masanao
M
Ito
Gukuto
G
Odawara
Chika
C
Yamasaki
Tomoteru
T
Kato
Koichi
K
Suzuki
Kazutoshi
K
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
D000081:Acetamides; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; C403132:Ro 64-0802; D053139:Oseltamivir