Groupe de Développements Méthodologiques en Tomographie par Emission de Positons, CEA/DSV/I2BM/CI-NAPS UMR6232, Université de Caen Basse Normandie, Caen, France.
J Med Chem. 2010 Feb 11;53(3):1281-7. doi: 10.1021/jm901550z.
The aim of the present investigation was to apply a chemical delivery system (CDS) to MIBG (4) with the purpose of delivering this drug to the CNS. Compound 4 has been linked to a 1,4-dihydroquinoline moiety in order to achieve its CNS penetration, and here we report the synthesis to link 4 to the chemical delivery system and the radiosynthesis with carbon-11 of the "CDS-4 entity". After iv injection into rats of the [(11)C]CDS-4, the follow-up study of the radioactivity distribution in blood samples and brain homogenates and the analysis by HPLC and LC-MS/MS have confirmed the release of 4 into the CNS.
本研究的目的是将一种化学传递系统 (CDS) 应用于 MIBG(4)，以便将该药物递送到中枢神经系统。为了实现其对中枢神经系统的穿透，化合物 4 已与 1,4-二氢喹啉部分相连，在此我们报告将 4 与化学传递系统连接的合成以及用碳-11 对“CDS-4 实体”的放射性合成。在大鼠静脉注射[(11)C]CDS-4 后，通过 HPLC 和 LC-MS/MS 对血液样本和脑匀浆中放射性分布的后续研究和分析，证实了 4 向中枢神经系统的释放。
