PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635

被引：61

作者：

Carson, RE ^{[1
]}

Lan, LX ^{[1
]}

Watabe, H ^{[1
]}

Der, MG ^{[1
]}

Adams, HR ^{[1
]}

Jagoda, E ^{[1
]}

Herscovitch, P ^{[1
]}

Eckelman, WC ^{[1
]}

机构：

[1] NIH, Warren Grant Magnuson Clin Ctr, PET Dept, Bethesda, MD 20892 USA

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 05期

关键词：

FCWAY; 5-HT1A receptors; modeling; volume of distribution;

D O I：

10.1016/S0969-8051(00)00118-9

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：

We synthesized [F-18]FCWAY, an analog of [carbonyl-C-11]WAY-100635 ([C-11]N-(2-(1-(4(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridinyl))cyclohexanecarboxamide}, by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [F-18]FC and [F-18]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [F-18]FCWAY has very similar kinetic characteristics to [C-11]WAY-100635. NUCL MED BIOL 27;5:493-497, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：493 / 497

页数：5

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