Motaleb M A, Ibrahem I T, Ayoub V R, Geneidi A S
Hot Labs Center, Egyptian Atomic Energy Authority, Cairo, Egypt.
Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
J Labelled Comp Radiopharm. 2016 Apr;59(4):147-52. doi: 10.1002/jlcr.3380. Epub 2016 Feb 23.
Noninvasive brain imaging is a process that allows scientists and physicians to view and monitor the areas of the brain. The aim of this study was to formulate a novel radiopharmaceutical for the detection of brain disorders at early stages in susceptible patients. (99m) Tc-ropinirole was prepared by the direct complexation of ropinirole with technetium-99m. The results showed that the radiochemical yield (99m) Tc-ropinirole was 92 ± 2.87% and the radiochemical yield was evaluated by paper chromatography and HPLC. In vitro studies showed that the formed complex was stable for up to 6 h. In vivo uptake of (99m) Tc-ropinirole in the brain was 4.87 ± 0.15% injected dose/g organ at 30 min post-injection, which cleared from the brain with time till it reaches 2.3% at 2 h post-injection indicating that the brain uptake of (99m) Tc-ropinirole is higher than that of the commercially available (99m) Tc-HMPAO, which is 2.25% at 30 min. Pre-dosing mice with cold ropinirole reduced the brain uptake to 0.26 ± 0.01% injected dose/g organ, so this confirms the high specificity and selectivity of this radiotracer for the assessment of the dopamine receptors.
无创脑成像是一种使科学家和医生能够观察和监测脑区的过程。本研究的目的是研制一种新型放射性药物，用于在易感患者中早期检测脑部疾病。（99m）Tc-罗匹尼罗是通过罗匹尼罗与99m锝直接络合制备的。结果表明，（99m）Tc-罗匹尼罗的放射化学产率为92±2.87%，放射化学产率通过纸色谱法和高效液相色谱法进行评估。体外研究表明，形成的络合物在长达6小时内稳定。注射后30分钟，（99m）Tc-罗匹尼罗在脑中的体内摄取量为4.87±0.15%注射剂量/克器官，随着时间的推移从脑中清除，在注射后2小时达到2.3%，这表明（99m）Tc-罗匹尼罗的脑摄取高于市售的（99m）Tc-HMPAO，后者在30分钟时为2.25%。用冷罗匹尼罗预先给药小鼠可将脑摄取量降低至0.26±0.01%注射剂量/克器官，因此这证实了这种放射性示踪剂对多巴胺受体评估具有高特异性和选择性。
