HIGH AFFINITY l‐[3H]GLUTAMATE BINDING TO POSTSYNAPTIC RECEPTOR SITES ON RAT CEREBELLAR MEMBRANES
HIGH AFFINITY l‐[3H]GLUTAMATE BINDING TO POSTSYNAPTIC RECEPTOR SITES ON RAT CEREBELLAR MEMBRANES
复制标题
高亲和力 l-[3H]谷氨酸与大鼠小脑膜上突触后受体位点的结合
作者：
A. C. Foster;P. Roberts
在源自大鼠小脑的膜制剂中研究了1[3H]谷氨酸结合，大鼠小脑是可能存在高密度突触后谷氨酸受体的大脑区域。谷氨酸是专门寻找的，在新鲜制备的膜中，在 pH 和温度的生理条件下是最佳的，并且与细胞的突触膜部分相关。特异性结合通过单一的高亲和力过程发生，KD 为 744 nM，容量为 73 pmol/mg 蛋白质。与 GABA 的研究结果不同，谷氨酸与新鲜膜的特异性结合不涉及摄取位点。对具有已知药理活性的多种化合物的效力进行比较，证明它们取代特异性谷氨酸结合的能力与与谷氨酸受体的特异性相互作用一致。
l[3H]glutamate binding was investigated in membrane preparations derived from rat cerebellum, an area of the brain where it is likely that a high density of postsynaptic glutamate receptors occurs. Glutamate was hound specifically and, in freshly prepared membranes, was optimal under physiological conditions of pH and temperature and was associated with the synaptic membrane fraction of the cell. Specific binding occurred through a single, high‐affinity process with a KD, of 744 nM and a capacity of 73 pmol/mg protein. Unlike the findings reported for GABA, the specific binding of glutamate to fresh membranes did not involve an uptake site. Comparison of the potencies of a wide range of compounds with known pharmacological activities, demonstrated that their ability to displace specific glutamate binding was consistent with specific interactions with glutamate receptors.