Synthesis of long-chain [¹⁸F]Deoxyfluoropoly(ethylene glycol) methyl ethers and their noninvasive pharmacokinetic analysis by positron emission tomography.
[¹⁸F]DeoxyfluoroPEG methyl ethers with an average molecular weight of 2 kDa ([¹⁸F]1a) and 10 kDa ([¹⁸F]1b) were synthesized by the fluorination of the tosylates 3a,b with [¹⁸F]nBu₄NF at 80°C for 20 min followed by flash filtration through a Sep-Pak Plus Alumina-N cartridge. After the intravenous administration of [¹⁸F]1a and [¹⁸F]1b to rats, their pharmacokinetics was analyzed by noninvasive, real-time, whole-living-body monitoring using positron imaging technology. The effect of PEG's molecular weight on their blood circulation and organ clearance were quantitatively visualized for the first time.
Department of Synthetic Organic Chemistry, Department of Medical Biochemistry, and Global COE Program, Graduate School of Pharmaceutical Sciences, University of Shizuoka, Yada, Suruga-ku, Shizuoka, Shizuoka 422-8526, Japan.
Shuji
S
Akai
Sho
S
Ishida
Kentaro
K
Hatanaka
Takayuki
T
Ishii
Norihiro
N
Harada
Hideo
H
Tsukada
Naoto
N
Oku
D000818:Animals; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D054879:Halogenation; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008738:Methyl Ethers / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods*; D051381:Rats; D017208:Rats, Wistar
D005462:Fluorine Radioisotopes; D008738:Methyl Ethers