锌离子增强了蜘蛛毒素（JSTX）合成类似物对谷氨酸受体的阻断效力。

Zinc ion enhances the blocking potency of synthetic analogs of spider toxin (JSTX) on the glutamate receptor.

作者信息

Kawai N, Miwa A, Hashimoto Y, Shudo K, Asami T, Nakajima T

机构信息

Department of Neurobiology, Tokyo Metropolitan Institute for Neurosciences, Japan.

出版信息

Neurosci Res. 1989 Apr;6(4):358-62. doi: 10.1016/0168-0102(89)90028-x.

DOI:10.1016/0168-0102(89)90028-x

PMID:2542850

Abstract

The effect of synthetic spider toxin analogs containing aza-crown in combination with zinc and copper was studied on the lobster neuromuscular synapse. The suppressive action of N4-type spider toxin analog (N4) on excitatory postsynaptic potentials (EPSPs) was markedly enhanced in the presence of 10(-5)-10(-4) M Zn2+. Cu2+ (10(-4) M) also had a potentiating effect on the suppression of EPSPs by N4 but to a lesser degree than Zn2+. While N6-type spider toxin analog (N6) suppressed EPSPs more effectively than N4, additional suppression was not pronounced in the presence of Zn2+ or Cu2+. The results suggest that chelatable divalent metal ions play an important role in the blocking mechanism of glutamate receptor by the spider toxin.

摘要

研究了含氮杂冠醚并结合锌和铜的合成蜘蛛毒素类似物对龙虾神经肌肉突触的作用。在存在10⁻⁵ - 10⁻⁴ M Zn²⁺的情况下，N4型蜘蛛毒素类似物（N4）对兴奋性突触后电位（EPSP）的抑制作用显著增强。Cu²⁺（10⁻⁴ M）对N4抑制EPSP也有增强作用，但程度小于Zn²⁺。虽然N6型蜘蛛毒素类似物（N6）比N4更有效地抑制EPSP，但在存在Zn²⁺或Cu²⁺时，额外的抑制作用并不明显。结果表明，可螯合的二价金属离子在蜘蛛毒素阻断谷氨酸受体的机制中起重要作用。