Shiue C Y, Shiue G G, Cornish K G, O'Rourke M F
Department of Radiology, University of Pennsylvania, Philadelphia 19104, USA.
Nucl Med Biol. 1995 Jul;22(5):613-6. doi: 10.1016/0969-8051(94)00146-b.
No-carrier-added [11C]fluoxetine (2) was synthesized by methylation of norfluoxetine (1) with [11C]H3I in 20% radiochemical yield in a synthesis time of 40 min from EOB with a specific activity of 0.48 Ci/microM (EOB). In vivo study in mouse indicated that the uptake of 2 in mouse tissues was high and the radioactivity remained constant throughout the study. The uptake of 2 in mouse brain was 4%/g. PET study in a Rhesus monkey also showed that the uptakes of 2 in different brain regions were similar and the retention of radioactivity in these regions remained constant throughout the study (80 min). Analysis of arterial plasma by HPLC showed that only 20% of radioactivity in the plasma remained as 2 at 30 min post-injection. These results suggest that the uptake of fluoxetine in monkey brain is probably not receptor mediated. Rather, blood flow, lipophilicity or other transport mechanisms may play a role in its uptake.
通过用[¹¹C]H₃I对去甲氟西汀（1）进行甲基化反应，在40分钟的合成时间内，以20%的放射化学产率从放化起始点（EOB）合成了无载体添加的[¹¹C]氟西汀（2），比活度为0.48 Ci/μM（EOB）。对小鼠的体内研究表明，2在小鼠组织中的摄取量很高，并且在整个研究过程中放射性保持恒定。2在小鼠脑中的摄取量为4%/克。对恒河猴的正电子发射断层扫描（PET）研究还表明，2在不同脑区的摄取量相似，并且在整个研究过程（80分钟）中这些区域的放射性滞留保持恒定。通过高效液相色谱法（HPLC）对动脉血浆进行分析表明，在注射后30分钟时，血浆中只有20%的放射性以2的形式存在。这些结果表明，氟西汀在猴脑中的摄取可能不是由受体介导的。相反，血流、亲脂性或其他转运机制可能在其摄取过程中起作用。
