Visualisation of 11C-flunitrazepam displacement in the brain of the live baboon
Visualisation of 11C-flunitrazepam displacement in the brain of the live baboon
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活狒狒大脑中 11C-氟硝西泮位移的可视化
DOI：
10.1097/00004728-198002000-00052
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发表时间：
1979
期刊：
影响因子：
64.8
通讯作者：
R. Naquet
中科院分区：
文献类型：
--
作者：
D. Comar;M. Maziére;J. M. GODOT;G. Berger;F. Soussaline;C. Menini;G. Arfel;R. Naquet
在体外实验中，大鼠1，2，狒狒3和人4，5的大脑中存在特异性苯二氮卓受体。在体内也观察到了地西泮6和氟硝西泮7的这些受体。然而，在此类实验中，尽管将放射性配体注射到活体动物中，但要证明特定受体的存在，需要对脑组织进行取样以进行体外定量测量。碳-11是一种半衰期为20分钟的正电子发射体，可用于非常高比活度的药物标记，这一事实提高了通过正电子发射断层扫描术在活体中进行放射性外部检测的可能性8，9。使用这种新的方法，本研究证明了11 C-氟硝西泮劳拉西泮在活狒狒的大脑中的位移。
THE presence of specific benzodiazepine receptors in the brain of rat1,2, baboon3 and man4,5 has been demonstrated in vitro. These receptors have also been observed in vivo for diazepam6 and flunitrazepam7. However in such experiments, although the radioactive ligand is injected in the living animal the demonstration of the presence of specific receptors requires brain tissue sampling for quantitative measurement in vitro. The fact that carbon-11 is a positron emitter with a half life of 20 min which can be used for very high specific activity labelling of drugs, raises the possibility of external detection of radioactivity in a living subject by positron emission tomography8,9. Using this new methodology the present study demonstrates te displacement of 11C-flunitrazepam by lorazepam in the brain of live baboons.