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The excitation of mammalian central neurones by amino acids.

机译:氨基酸激发哺乳动物中枢神经元。

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摘要

1. The relative potencies of a number of analogues of L-glutamate as excitants of thalamic neurones in the rat have been compared. The most powerful compounds were kainate, ibotenate and (+/-)cis-1-amino-1,3-dicarboxycyclopentane. The D- and L-isomers of glutamate and aspartate were also compared. Whereas D-glutamate is approximately one-half as active as the L-form, D-aspartate is more potent than L-aspartate. 2. Computer analysis has indicated that ibotenate and cis-1-amino-1,3-dicarboxy-cyclopentane have relatively fixed and similar C alpha-N, Comega-N and C alpha-Comega interatomic distances which can also be achieved by glutamate in certain conformations of the molecule, but not by aspartate. 3. Parallel examination of the antagonists glutamate diethylester and D-alpha-aminoadipate has shown that the former preferentially reduces L-glutamate effects while the latter blocks the actions of other amino acid excitants more readily than those of L-glutamate. 4. The evidence is consistent with the hypothesis that at least two populations of neuronal receptors for the excitatory amino acids exist.
机译:1.比较了大鼠中多种L-谷氨酸类似物作为丘脑神经元兴奋剂的相对效力。最有效的化合物是海藻酸盐,异丁酸酯和(+/-)顺式-1-氨基-1,3-二羧基环戊烷。还比较了谷氨酸和天冬氨酸的D-和L-异构体。 D-谷氨酸的活性大约是L-形式的一半,而D-天冬氨酸的效力比L-天冬氨酸强。 2.计算机分析表明,依博替尼酸酯和顺式-1-氨基-1,3-二羧基-环戊烷具有相对固定且相近的C alpha-N,Comega-N和C alpha-Comega原子间距离,谷氨酸在分子的某些构象,但不是天冬氨酸。 3.对拮抗剂谷氨酸二乙酯和D-α-氨基己二酸酯的平行检查显示,前者优先降低L-谷氨酸的作用,而后者比L-谷氨酸更容易阻止其他氨基酸兴奋剂的作用。 4.证据与以下假设一致:存在至少两个兴奋性氨基酸的神经元受体。

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