3-羟基-2-喹喔啉羧酸（一种新发现的兴奋性氨基酸拮抗剂）的抗惊厥特性

Anticonvulsant properties of 3-hydroxy-2-quinoxalinecarboxylic acid, a newly found antagonist of excitatory amino acids.

作者信息

Erez U, Frenk H, Goldberg O, Cohen A, Teichberg V I

出版信息

Eur J Pharmacol. 1985 Mar 26;110(1):31-9. doi: 10.1016/0014-2999(85)90025-1.

Abstract

Various aromatic acids have been investigated as putative ligands of excitatory amino acid receptors. 3-Hydroxy-2-quinoxalinecarboxylic acid (HQC), at 1 mM, was found to antagonize the 22Na+ efflux produced in 22Na+-preloaded brain slices by N-methyl-D-aspartate and kainate. The response to glutamate was also affected but not that to quisqualate. The apparent KI value of HQC for suppression of the N-methyl-D-aspartate response was 0.27 mM. The anticonvulsant action of HQC was investigated in mice and rats. HQC administered intracerebroventricularly caused a dose dependent delay in the occurrence of picrotoxin induced convulsions and afforded protection against picrotoxin induced death. These results confirm the proposition that antagonists of excitatory amino acids possess anticonvulsant properties.

摘要

多种芳香酸已被作为兴奋性氨基酸受体的假定配体进行研究。发现1 mM的3-羟基-2-喹喔啉羧酸（HQC）可拮抗N-甲基-D-天冬氨酸和红藻氨酸在预加载22Na+的脑片中产生的22Na+外流。对谷氨酸的反应也受到影响，但对喹啉酸的反应未受影响。HQC抑制N-甲基-D-天冬氨酸反应的表观抑制常数（KI）值为0.27 mM。在小鼠和大鼠中研究了HQC的抗惊厥作用。脑室内给予HQC会导致印防己毒素诱导惊厥的发生出现剂量依赖性延迟，并提供针对印防己毒素诱导死亡的保护作用。这些结果证实了兴奋性氨基酸拮抗剂具有抗惊厥特性这一观点。