PET studies of 18F-memantine in healthy volunteers
PET studies of 18F-memantine in healthy volunteers
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DOI：
10.1016/s0969-8051(01)00293-1
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发表时间：
2002-02-01
影响因子：
3.1
通讯作者：
Schubiger, PA
中科院分区：
文献类型：
--
作者：
Ametamey, SM;Bruehlmeier, M;Schubiger, PA
先前对小鼠的研究和对恒河猴的 PET 研究表明，药理学剂量的美金刚和 (+)-MK-801 可以阻断 F-18-美金刚的局部摄取。在本研究中，在五名健康志愿者中检查了 F-18-美金刚的结合特性。在人类中。 F-18-美金刚均匀分布在灰质中，即皮质和基底神经节区域以及小脑中。在 PET 研究期间，血浆中未检测到放射性代谢物。 F-18-美金刚在富含受体的重离子（例如纹状体和额叶皮层）中的摄取可以通过 1 组织室模型很好地描述。所有灰质区域的 DV" 值相似，范围为 15 至 20 ml/ml。白质显示较低的 DV" 值，为 15 +/- 1.4 ml/ml。这些结果表明，F-18-美金刚在人脑中的分布并不反映区域NMDA受体浓度，因此，该放射性配体不适合NMDA受体的PET成像。 (C) 2002 Elsevier Science Inc. 保留所有权利。
Previous studies in mice and PET investigations in a Rhesus monkey showed that the regional uptake of F-18-memantine could be blocked by pharmacological doses of memantine and (+)-MK-801. In the present study, the binding characteristics of F-18-memantine was examined in five healthy volunteers.In humans. F-18-memantine was homogeneously distributed in gray matter i.e. cortex and basal ganglia regions, as well as the cerebellum. No radioactive metabolites were detected in plasma during the time-frame of the PET studies. The uptake of F-18-memantine in receptor-rich re-ions such as striatum and frontal cortex could be well described by a 1-tissue compartment model. The DV" values of all gray matter regions were similar and ranged from 15 to 20 ml/ml. The white matter showed lower DV" values of 15 +/- 1.4 ml/ml. These results suggest that F-18-memantine distribution in human brain does not reflect the regional NMDA receptor concentration, and therefore, this radioligand is not suitable for the PET imaging of the NMDA receptors. (C) 2002 Elsevier Science Inc. All rights reserved.