Application of a novel phenylpiperazine formation reaction to the radiosynthesis of a model fluorine-18-labeled radiopharmaceutical ((FTFMPP)-F-18)

被引：11

作者：

Mishani, E ^{[1
]}

Cristel, ME ^{[1
]}

Dence, CS ^{[1
]}

McCarthy, TJ ^{[1
]}

Welch, MJ ^{[1
]}

机构：

[1] WASHINGTON UNIV,SCH MED,EDWARD MALLINCKRODT INST RADIOL,DIV RADIOL SCI,ST LOUIS,MO 63110

来源：

NUCLEAR MEDICINE AND BIOLOGY | 1997年 / 24卷 / 03期

关键词：

serotonin; TFMPP; F-18]fluoride; phenylpiperazine;

D O I：

10.1016/S0969-8051(97)00063-2

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

The labeled serotonin agonist 3-[F-18]fluoro-N-(alpha,alpha,alpha-trifluoro-m-tolyl)piperazine ((FTFMPP)-F-18) was prepared rapidly using the labeling procedure for trifluorotoluenes, [F-18]fluoro-for-nitro exchange, followed by an alumina-supported bis-alkylation. After normal-phase HPLC purification, the labeled product was obtained in 20-32% (n = 20) decay-corrected radiochemical yield with a radiochemical purity >98% and a specific activity of 100 GBq/mu mol. The synthesis time including purification was 3 h. The receptor binding affinity of FTFMPP to rat brain membranes was found to be similar to that of the nonfluorinated parent compound (TFMPP). Although TFMPP has been proposed by others as an agent for the imaging of serotonin receptors, only minimal receptor-mediated uptake was observed. (C) 1997 Elsevier Science Inc.

引用

页码：269 / 273

页数：5

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