Carson R E, Lang L, Watabe H, Der M G, Adams H R, Jagoda E, Herscovitch P, Eckelman W C
Positron Emission Tomography Department, Warren Grant Magnuson Clinical Center, National Institutes of Health, Building 10, Room 1C-401, 10 Center Dr., MSC 1180, Bethesda, Maryland 20892-1180, USA.
Nucl Med Biol. 2000 Jul;27(5):493-7. doi: 10.1016/s0969-8051(00)00118-9.
We synthesized [(18)F]FCWAY, an analog of [carbonyl-(11)C]WAY-100635 ¿[(11)C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridi nyl))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 [(18)F]FC and [(18)F]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 [(18)F]FCWAY has very similar kinetic characteristics to [(11)C]WAY-100635.
我们合成了[(18)F]FCWAY，它是[羰基-(11)C]WAY-100635（即[(11)C]N-(2-(1-(4-(2-甲氧基苯基)-哌嗪基)乙基))-N-(2-(吡啶基))环己烷甲酰胺）的类似物，通过用反式-4-氟环己烷羰基（FC）取代环己烷羰基酸得到。在麻醉的猴子身上进行了对照和预阻断研究。血浆放射性代谢物分析显示存在[(18)F]FC和[(18)F]氟化物。基于对这两种标记代谢物的单独正电子发射断层扫描研究，对组织时间-放射性曲线进行了代谢物污染校正。使用双组织室模型进行分析得到的分布容积（V）估计值（mL/mL）范围从额叶皮质的33到小脑的4。预阻断数据显示V均匀为2 - 3 mL/mL。这些研究表明[(18)F]FCWAY具有与[(11)C]WAY-100635非常相似的动力学特征。
Zotero 插件