Shiue C Y, Teng R R, Bai L Q, Wolf A P, Arnett C D, Simon E J
Int J Rad Appl Instrum B. 1987;14(2):119-22. doi: 10.1016/0883-2897(87)90141-3.
No-carrier-added (NCA) (+/-)-N-(3-[18F]Fluoropropyl)-N-normetazocine (2) was synthesized by N-alkylation of (+/-)-N-normetazocine (1) with NCA 1-[18F]fluoro-3-iodopropane in an overall radiochemical yield of 10% (EOB) with a mass of 3.5 nmol in a synthesis time of 90 min from end of bombardment (EOB). PET studies of 2 in a baboon did not indicate specificity for opiate receptor sites alone: The activity declined rapidly in the striatum, the frontal cortex and the cerebellum. The baboon total arterial plasma radioactivity clearance was very rapid and the metabolism of compound 2 in plasma was also very rapid. These results suggest that compound 2 is not a suitable radioligand for imaging opiate receptors in the human brain by positron tomography.
通过将（±）-N-去甲美他唑辛（1）与无载体添加（NCA）的1-[¹⁸F]氟-3-碘丙烷进行N-烷基化反应，合成了无载体添加（NCA）的（±）-N-（3-[¹⁸F]氟丙基）-N-去甲美他唑辛（2），从轰击结束（EOB）开始，在90分钟的合成时间内，总放射化学产率为10%（按注射结束时计算），质量为3.5 nmol。在狒狒身上对2进行的正电子发射断层扫描（PET）研究并未表明其仅对阿片受体位点具有特异性：纹状体、额叶皮质和小脑中的活性迅速下降。狒狒的总动脉血浆放射性清除非常迅速，化合物2在血浆中的代谢也非常迅速。这些结果表明，化合物2不是通过正电子断层扫描在人脑中成像阿片受体的合适放射性配体。
