Luini A, Tal N, Goldberg O, Teichberg V I
Brain Res. 1984 Dec 24;324(2):271-7. doi: 10.1016/0006-8993(84)90037-4.
Searching for the endogenous ligands of the 4 classes of excitatory amino acid receptors detected in the mammalian CNS, we have measured, using a 22Na+ efflux receptor assay, the excitatory activity of 42 brain constituents or analogs and established the receptor specificity of those substances which possess excitatory properties. Among the substances tested were methyltetrahydrofolate and N-acetylaspartylglutamate, two putative ligands of the kainate and glutamate receptors. These compounds were found to have very little or no excitatory activity, respectively. The 8 brain constituents possessing excitatory properties displayed a receptor specificity similar to either that of N-methyl-D-aspartate (e.g. quinolinate) or glutamate (e.g. cysteine sulfinate) but not of kainate or quisqualate. These results are discussed in relation with the problem of the identification of brain excitatory neurotransmitters.
为寻找在哺乳动物中枢神经系统中检测到的4类兴奋性氨基酸受体的内源性配体,我们使用22Na+外流受体分析法测定了42种脑成分或类似物的兴奋性活性,并确定了那些具有兴奋性特性的物质的受体特异性。所测试的物质包括甲基四氢叶酸和N-乙酰天冬氨酰谷氨酸,它们分别是海人藻酸受体和谷氨酸受体的两种假定配体。结果发现,这些化合物分别几乎没有或根本没有兴奋性活性。具有兴奋性特性的8种脑成分显示出与N-甲基-D-天冬氨酸(如喹啉酸)或谷氨酸(如半胱氨酸亚磺酸盐)相似但与海人藻酸或quisqualate不同的受体特异性。结合脑兴奋性神经递质的鉴定问题对这些结果进行了讨论。