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源自海藻酸的肽作为大鼠脑中N-甲基-D-天冬氨酸诱导的神经兴奋的拮抗剂。

Peptides derived from kainic acid as antagonists of N-methyl-D-aspartate-induced neuroexcitation in rat brain.

作者信息

Goldberg O, Teichberg V I

出版信息

Neurosci Lett. 1985 Sep 16;60(1):101-5. doi: 10.1016/0304-3940(85)90388-x.

Abstract

The effects of dipeptides and an amide chemically derived from kainic acid (KA) on the response of rat striatal slices to excitatory amino acids were studied. Some of the gamma-peptides of KA were found to antagonize the response to N-methyl-D-aspartate (NMDA) more than that to quisqualate and glutamate and not to have any effect on the response to kainate. The least potent antagonists among the tested compounds were the gamma-amide of KA and the peptides of KA with beta-alanine and gamma-aminobutyric acid, whereas the gamma-kainyl peptides of the alpha-amino acids glycine, tyrosine, glutamate and KA were more active. The latter are the best blockers of the response to NMDA among the tested compounds.

摘要

研究了二肽以及一种由海藻酸(KA)化学衍生的酰胺对大鼠纹状体切片对兴奋性氨基酸反应的影响。发现一些KA的γ-肽对N-甲基-D-天冬氨酸(NMDA)反应的拮抗作用比对喹啉酸和谷氨酸的拮抗作用更强,且对海人藻酸反应无任何影响。在所测试的化合物中,活性最弱的拮抗剂是KA的γ-酰胺以及含β-丙氨酸和γ-氨基丁酸的KA肽,而含α-氨基酸甘氨酸、酪氨酸、谷氨酸和KA的γ-海人藻酰肽活性更高。在测试的化合物中,后者是对NMDA反应的最佳阻断剂。

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