Demonstration of [3H] diazepam binding to benzodiazepine receptors in vivo.
Demonstration of [3H] diazepam binding to benzodiazepine receptors in vivo.
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证明[3H]地西泮在体内与苯二氮卓受体结合。
DOI：
10.1016/0024-3205(78)90560-x
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发表时间：
1978
期刊：
影响因子：
6.1
通讯作者：
P. Skolnick
中科院分区：
文献类型：
--
作者：
M. J. Williamson;S. Paul;P. Skolnick
大鼠静脉注射苯二氮卓受体后用[3h]地西泮标记。[3h]地西泮在体内与大鼠前脑膜的结合可通过氯西泮或两种苯二氮卓类药物B9和B10的药理活性对映体进行置换，但不能通过等剂量的药理活性对映体进行置换。[3h]地西泮在体内的结合在肾脏、肝脏和腹肌中被观察到，但在任何研究的外周组织中没有立体特异性移位。苯二氮卓类受体在大脑中的区域分布不均匀，[3h]地西泮特异性结合在大脑皮层最高，在脑髓最低。[3h]地西泮结合的亚细胞分布的初步研究表明，与突触体膜的结合具有最高的特异性。这些数据证明了在大鼠脑内标记苯二氮卓受体的可行性。
Benzodiazepine receptors were labeled with [3 H] diazepam following intravenous injection in rats. Binding of [3 H] diazepam in vivo to rat forebrain membranes was displaceable by co-injection of clonazepam or the pharmacologically active enantiomers of two benzodiazepines, B9 and B10, but was not displaced by equal doses of the pharmacologically in-active enantiomers. Binding of [3 H] diazepam in vivo was bserved in kidney, liver, and abdominal muscle, but was not stereospecifically diplaced in any peripheral tissue studied. The regional distribution of benzodiazepine receptors in brain was uneven, with specific [3 H] diazepam binding being highest in the cerebral cortex and lowest in the ponsmedulla. Preliminary studies of the subcellular distribution of [3 H] diazepam binding demonstrated highest specific binding to synaptosomal membranes. These data demonstrate the feasibility of labeling benzodiazepine receptors in rat brain in vivo.