Synthesis of a 11C-labelled derivative of the N-methyl-D-aspartate receptor antagonist MK-801

被引：0
|
作者：
Andersson, Y
Tyrefors, N
Sihver, S
Onoe, H
Watanabe, Y
Tsukada, H
Langstrom, B [1 ]
机构：
[1] Univ Uppsala, PET Ctr, UAS, S-75185 Uppsala, Sweden
[2] JST, Subfemtomole Biorecognit Project, Uppsala, Sweden
[3] Osaka Biosci Inst, Dept Neurosci, Osaka, Japan
[4] Hamamatsu Photon, Cent Res Lab, Hamakita, Japan
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1998年 / 41卷 / 06期
关键词：
NMDA-receptor; MK-801; palladium-promoted C-11-cyanation; C-11]cyano-MK-801; positron emission tomography; in vivo investigation;
D O I：
10.1002/(SICI)1099-1344(199806)41:6<567::AID-JLCR96>3.0.CO;2-8
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
A one-pot synthesis of (+)-3-[C-11]cyano-MK-801 was performed using a palladium-promoted reaction of hydrogen [C-11]cyanide with (+)-3-iodo-MK-801. The synthesis time was 32 min counted from end of bombardment, affording (+)-3-[C-11]cyano-MK-801 in 37 % decay-corrected radiochemical yield based on hydrogen [C-11]cyanide. The radiochemical purity was higher than 95 % and the specific radioactivity was in the range of 220-600 GBq/mu mol. In vitro investigations in homogenate and frozen sections of rat brain indicated that (+)-3-[C-11]cyano-MK-801 may be used as tracer in studies of the NMDA receptor.
引用
收藏
页码：567 / 576
页数：10
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