[11C]R116301作为人体NK1受体体内示踪剂的首次评估。
First evaluation of [11C]R116301 as an in vivo tracer of NK1 receptors in man.
作者信息
Wolfensberger Saskia P A, van Berckel Bart N M, Airaksinen Anu J, Maruyama Kaoru, Lubberink Mark, Boellaard Ronald, Carey William D H, Reddingius Wieb, Veltman Dick J, Windhorst Albert D, Leysen Josée E, Lammertsma Adriaan A
机构信息
Department of Nuclear Medicine & PET Research, VU University Medical Centre, P.O. BOX 7057, 1007 MB, Amsterdam, The Netherlands.
出版信息
Mol Imaging Biol. 2009 Jul-Aug;11(4):241-5. doi: 10.1007/s11307-009-0204-5. Epub 2009 Mar 31.
PURPOSE
NK1 receptors have been implicated in various neuropsychiatric and other disorders. R116301 is a selective NK1 receptor antagonist. In this pilot study, [(11)C]R116301 was evaluated as a potential positron emission tomography (PET) ligand for the NK1 receptor.
PROCEDURES
Two dynamic PET studies were performed in three normal volunteers before and after a blocking dose of aprepitant. Data were analyzed using striatum to cerebellum standardized uptake value (SUV) ratios.
RESULTS
Baseline SUV ratios at 60-90 min after injection ranged from 1.22 to 1.70. Following aprepitant administration, this specific signal was completely blocked. Aprepitant administration did not significantly affect uptake in cerebellum, confirming the absence of NK1 receptors in cerebellum.
CONCLUSION
These preliminary results indicate that [(11)C]R116301 has potential as a radioligand for in vivo assessment of NK1 receptors in the human brain.
目的
NK1受体与多种神经精神疾病及其他病症有关。R116301是一种选择性NK1受体拮抗剂。在这项初步研究中，[（11）C]R116301被评估为一种用于NK1受体的潜在正电子发射断层扫描（PET）配体。
程序
在三名正常志愿者中，于给予阿瑞匹坦阻断剂量前后进行了两项动态PET研究。使用纹状体与小脑标准化摄取值（SUV）比值分析数据。
结果
注射后60 - 90分钟的基线SUV比值在1.22至1.70之间。给予阿瑞匹坦后，这种特异性信号被完全阻断。给予阿瑞匹坦并未显著影响小脑的摄取，证实小脑中不存在NK1受体。
结论
这些初步结果表明，[（11）C]R116301有潜力作为一种放射性配体用于体内评估人脑中的NK1受体。
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