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Radiosynthesis of [ 18 F]N‐(4‐phenylbutyl)‐4‐(4‐fluorobenzoyl)piperidine for studying serotonin 5‐HT 2a receptors
Author(s) -
Hashimoto Kenji,
Hatano Kentaro,
Minabe Yoshio,
Iyo Masaomi,
Taniguchi Masahiko,
Hoshino Osamu,
Sakiyama Yojiro,
Kawasumi Yasuhiro
Publication year - 1998
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(1998100)41:10<941::aid-jlcr151>3.0.co;2-6
Subject(s) - chemistry , radiosynthesis , piperidine , serotonin , in vivo , specific activity , receptor , nucleophile , yield (engineering) , high performance liquid chromatography , radiochemistry , 5 ht receptor , nuclear chemistry , stereochemistry , chromatography , organic chemistry , biochemistry , materials science , microbiology and biotechnology , metallurgy , biology , enzyme , catalysis
N‐(4‐Phenylbutyl)‐4‐(4‐fluorobenzoyl)piperidine [4‐PBFBP] shows highly selective binding to serotonin 5‐HT 2A receptors with high affinity. In this study, we prepared [ 18 F]4‐PBFBP for in vivo study of 5‐HT 2A receptors in the brain using positron emission tomography (PET). Nucleophilic aromatic displacement of N‐(4‐phenylbutyl)‐4‐(4‐nitrobenzoyl)piperidine by no carrier added [ 18 F]fluoride which was solubilized by Kryptofix 222 in DMSO produced [ 18 F]4‐PBFBP with high specific radioactivity. The product was purified by reversed phase preparative HPLC and was extracted from the collected eluate by SEP‐PAK ® C18 cartridge prior to formulation. The radiochemical yield of the final product was 15±1.8% (mean±S.D. of three experiments) with decay correction and the specific activity was 113±27 GBq/ μmol (mean±S.D. of three experiments) at E.O.S. after a total preparation time of about 160 min. The radiochemical purity of [ 18 F]4‐PBFBP was more than 99%. The regional distribution of [ 18 F]4‐PBFBP in mouse brain was also examined.Copyright © 1998 John Wiley & Sons, Ltd.