新合成的蜘蛛毒素类似物可阻断甲壳类动物的谷氨酸受体。

Newly synthesized analogues of the spider toxin block the crustacean glutamate receptor.

作者信息

Shudo K, Endo Y, Hashimoto Y, Aramaki Y, Nakajima T, Kawai N

机构信息

Department of Organic Chemistry, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.

出版信息

Neurosci Res. 1987 Oct;5(1):82-5. doi: 10.1016/0168-0102(87)90026-5.

DOI:10.1016/0168-0102(87)90026-5

PMID:2829068

Abstract

Effects of synthetic compounds similar to the structure of a spider toxin were studied on the glutamate receptors in crustacean neuromuscular synapses. Two kinds of analogues, 2,4-dihydroxyphenylacetyl-asparaginyl cadaverine (C-1) and 2,4-dihydroxyphenylacetyl-asparaginyl spermine (C-2), suppressed the excitatory postsynaptic potentials in a manner similar to natural spider toxin (JSTX). The dose-response relationship showed that the relative potency of the compounds is C-1 less than C-2 less than JSTX. While the effect of JSTX was irreversible, those of C-1 and C-2 were reversible. These synthetic compounds may serve as important tools in studying the structure and function of glutamate receptors.

摘要

研究了结构与蜘蛛毒素相似的合成化合物对甲壳类动物神经肌肉突触中谷氨酸受体的影响。两种类似物，2,4-二羟基苯乙酰-天冬酰胺基尸胺（C-1）和2,4-二羟基苯乙酰-天冬酰胺基精胺（C-2），以类似于天然蜘蛛毒素（JSTX）的方式抑制兴奋性突触后电位。剂量-反应关系表明，这些化合物的相对效力为C-1小于C-2小于JSTX。虽然JSTX的作用是不可逆的，但C-1和C-2的作用是可逆的。这些合成化合物可能成为研究谷氨酸受体结构和功能的重要工具。