A subclass of GABA(A)/benzodiazepine receptor exclusively localized in the limbic system
A subclass of GABA(A)/benzodiazepine receptor exclusively localized in the limbic system
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DOI：
10.1097/00001756-199612200-00024
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发表时间：
1996-12-20
期刊：
影响因子：
1.7
通讯作者：
Watanabe, Y
中科院分区：
文献类型：
--
作者：
Onoe, H;Tsukada, H;Watanabe, Y
使用具有高比放射性（> 70 GBq mu mol(-1)）的C-11标记的Ro15-4513进行的体内饱和研究揭示了γ-氨基丁酸A型/苯二氮卓（GABA(A)/BZ）受体中存在极高亲和力和高亲和力结合位点（杏仁核中的K-d值分别类似于0.4和18.7 nM）。活猴脑。将使用[C-11]Ro15-4513获得的低比放射性图像与高比放射性图像（两者均使用高空间分辨率正电子发射断层扫描相机扫描）相减，证明极高亲和力位点仅位于边缘系统，例如杏仁核、海马、前扣带回、隔膜、伏隔核和岛叶皮层。非常高亲和力的结合位点的定位可能源自中央 GABA(A)/BZ 受体的一个亚类，这可能解释了 BZ 类似物的抗焦虑作用。
AN in vivo saturation study using C-11-labelled Ro15-4513 with high specific radioactivity (> 70 GBq mu mol(-1)) revealed the presence of very high-affinity and high-affinity binding sites (K-d values in the amygdala similar to 0.4 and 18.7 nM, respectively) in the gamma-aminobutyric acid type A/benzodiazepine (GABA(A)/BZ) receptor in the living monkey brain. Subtraction of an image obtained using [C-11]Ro15-4513 with low specific radioactivity from an image obtained by that with high specific radioactivity, both of which were scanned with a high spatial resolution positron emission tomography camera, demonstrated that the very high-affinity sites are exclusively localized in the limbic system, such as in the amygdala, hippocampus, anterior cingulate, septum, nucleus accumbens and insular cortex. The localization of the very high-affinity binding sites, which may be derived from a subclass of central GABA(A)/BZ receptors, might account for the anxiolytic effect of BZ analogues.