title: Optimization of the radiosynthesis of [(18) F]MEFWAY for imaging brain serotonin 1A receptors by using the GE TracerLab FXFN-Pro module.
abstract: The aim of this study was to develop a highly reliable radiofluorination method for the preparation of N-{2-[4-(2-methoxyphenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(4-(18) F-fluoromethylcyclohexane)carboxamide ([(18) F]Mefway) by using a fully automated system. The optimal condition is composed of two parts. The extraction system of the trapped F-18 in the anion exchange resin (i.e., quaternary methylamine cartridge) is a complex of Kryptofix 2.2.2. (K222, 4 mg/0.9 mL methanol) and K2 CO3 (1 mg/0.1 mL H2 O). After removing the solvents, the trans-tosylated Mefway precursor (1 mg/0.5 mL acetonitrile) was reacted with dried K222-K[(18) F] at 100°C for 5 min. After purification and formulation, [(18) F]Mefway was obtained with 38 ± 2.4% (decay corrected, n = 34) radiochemical yield, a total synthesis time of 52 ± 3.4 min, specific activity was 120.6 ± 8.7 GBq/µmol at the end of synthesis and a radiochemical purity of 99%. According to the quality control tests, formulated [(18) F]Mefway is suitable to apply parenteral clinical application.
authors.affiliation: Department of Nuclear Medicine, Yonsei University College of Medicine, Gangnam Severance Hospital, Seoul, 135-720, Korea.
authors.forename: Jae Yong
authors.initials: JY
authors.lastname: Choi
authors.forename: Chul Hoon
authors.initials: CH
authors.lastname: Kim
authors.forename: Young Hoon
authors.initials: YH
authors.lastname: Ryu
authors.forename: Young Beom
authors.initials: YB
authors.lastname: Seo
authors.forename: Phong
authors.initials: P
authors.lastname: Truong
authors.forename: Eun Jung
authors.initials: EJ
authors.lastname: Kim
authors.forename: Tae Hyun
authors.initials: TH
authors.lastname: Choi
authors.forename: JeeHae
authors.initials: J
authors.lastname: Kang
authors.forename: Minkyung
authors.initials: M
authors.lastname: Lee
authors.forename: Dong Goo
authors.initials: DG
authors.lastname: Kim
authors.forename: Jong Doo
authors.initials: JD
authors.lastname: Lee
authors.forename: Tae Joo
authors.initials: TJ
authors.lastname: Jeon
mesh_terms: D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D010879:Piperazines / Q000138:chemical synthesis*; D011725:Pyridines / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: D005462:Fluorine Radioisotopes; D010879:Piperazines; D011725:Pyridines; D019275:Radiopharmaceuticals; C515664:mefway
keywords: Mefway; PET; automated radiosynthesis; serotonin 1A receptor