Treyer Valerie, Streffer Johannes, Ametamey Simon M, Bettio Andrea, Bläuenstein Peter, Schmidt Mark, Gasparini Fabrizio, Fischer Uta, Hock Christoph, Buck Alfred
PET Center, Division of Nuclear Medicine, University Hospital Zurich, Zurich, Switzerland.
Eur J Nucl Med Mol Imaging. 2008 Apr;35(4):766-70. doi: 10.1007/s00259-007-0638-4. Epub 2007 Dec 11.
In this study, we assessed the whole-body biodistribution and radiation dosimetry of the new glutamatergic ligand (11)C-ABP688. This ligand binds specifically to the metabotropic glutamatergic receptor of subtype 5 (mGluR5).
The study included five healthy male volunteers aged 20-29 years. After intravenous injection of 240-260 MBq, a series of four to ten whole-body positron emission tomography/computed tomography scans were initiated, yielding 60-80 min of data. Residence times were then calculated in the relevant organs, and the software packages Mirdose and Olinda were used to calculate the absorbed radiation dose and the effective dose equivalent.
Of the excreted (11)C activity at 1 hour, approximately 80% were eliminated via the hepato-biliary pathway and 20% through the urinary tract. The absorbed dose (mGy/MBq) was highest in the liver (1.64 E (-2) +/- 5.08 E (-3)), gallbladder (8.13 E (-3) +/- 5.6 E (-3)), and kidneys (7.27 E (-3) +/- 2.79 E (-3)). The effective dose equivalent was 3.68 +/- 0.84 microSv/MBq. Brain uptake in the areas with high mGluR5 density was 2-3 (SUV). The agreement between the values obtained from Mirdose and the Olinda was excellent.
(11)C-ABP688 is a very promising ligand for the investigation of mGluR5 receptors in humans. Brain uptake is high and the effective dose equivalent so low that serial examinations in the same subject seem feasible.
在本研究中，我们评估了新型谷氨酸能配体（11）C - ABP688的全身生物分布和辐射剂量学。该配体特异性结合5型代谢型谷氨酸能受体（mGluR5）。
该研究纳入了5名年龄在20 - 29岁的健康男性志愿者。静脉注射240 - 260 MBq后，开始进行一系列四至十次全身正电子发射断层扫描/计算机断层扫描，获取60 - 80分钟的数据。然后计算相关器官的滞留时间，并使用Mirdose和Olinda软件包计算吸收辐射剂量和有效剂量当量。
在1小时时排泄的（11）C活度中，约80%通过肝胆途径消除，20%通过尿路消除。肝脏（1.64 E（-2）±5.08 E（-3））、胆囊（8.13 E（-3）±5.6 E（-3））和肾脏（7.27 E（-3）±2.79 E（-3））的吸收剂量（mGy/MBq）最高。有效剂量当量为3.68±0.84微Sv/MBq。mGluR5密度高的区域的脑摄取为SUV的2 - 3倍。Mirdose和Olinda获得的值之间的一致性非常好。
（11）C - ABP688是用于研究人类mGluR5受体的非常有前景的配体。脑摄取高且有效剂量当量低，以至于在同一受试者中进行系列检查似乎是可行的。
