Takahashi K, Murakami M, Miura S, Iida H, Kanno I, Uemura K
Department of Radiology and Nuclear Medicine, Research Institute for Brain and Blood Vessels-Akita, Japan.
Appl Radiat Isot. 1999 Mar;50(3):521-5. doi: 10.1016/s0969-8043(97)10155-5.
(+)N-[11C]methyl-3-piperidyl benzilate, a relatively low affinity muscarinic cholinergic receptor antagonist was synthesized by N-[11C]methylation of (+)3-piperidyl benzilate using [11C]methyl iodide. The product was isolated by HPLC, and obtained with radiochemical yield of 60-70% from [11C]methyl iodide, and a specific activity of 500-1000 Ci mmol-1 (18.5-37 GBq mumol-1) at EOS and radiochemical purity of > 98%. In vitro autoradiographic studies showed selective binding for this radiotracer in the different regions of the rat brain: high in corpus striatum, hippocampus and cerebral cortex, and low in cerebellum, consistent with muscarinic cholinergic receptor distributions. This radiotracer thus had potential as radioligand for positron emission tomography.
（+）N - [¹¹C]甲基 - 3 - 哌啶基苯甲酸苄酯是一种亲和力相对较低的毒蕈碱型胆碱能受体拮抗剂，它通过使用[¹¹C]碘甲烷对（+）3 - 哌啶基苯甲酸苄酯进行N - [¹¹C]甲基化反应合成。产物通过高效液相色谱法分离，以[¹¹C]碘甲烷计，放射化学产率为60 - 70%，在放射性核素显像结束时比活度为500 - 1000 Ci mmol⁻¹（18.5 - 37 GBq μmol⁻¹），放射化学纯度> 98%。体外放射自显影研究表明，这种放射性示踪剂在大鼠脑的不同区域有选择性结合：纹状体、海马和大脑皮质中含量高，小脑含量低，这与毒蕈碱型胆碱能受体分布一致。因此，这种放射性示踪剂有潜力作为正电子发射断层扫描的放射性配体。
