N-苯磺酰基磷酰二胺酯类化合物的合成及其对昆虫谷氨酸受体通道阻断作用的研究

高等学校化学学报 ›› 1995, Vol. 16 ›› Issue (8): 1215.

N-苯磺酰基磷酰二胺酯类化合物的合成及其对昆虫谷氨酸受体通道阻断作用的研究

陈茹玉, 戴庆, 王惠林, 刘安西, 赵勇

南开大学元素有机化学研究所, 天津, 300071

收稿日期:1994-09-17 修回日期:1995-03-25 出版日期:1995-08-24 发布日期:1995-08-24
通讯作者: 陈茹玉,女,75岁,教授.
作者简介:陈茹玉,女,75岁,教授.
基金资助:
国家自然科学基金

Synthesis of N-Phenylsulfonyl Phosphordiamides and Study on Effects of Structures on Insect Glutamate Potentials

CHEN Ru-Yu, DAI Qing, WANG Hui-Lin, LIU An-Xi, ZHAO Yong

Institute of Elemento-Organic Chemistry, Tianjin, 300071

Received:1994-09-17 Revised:1995-03-25 Online:1995-08-24 Published:1995-08-24

摘要/Abstract

摘要： 报道了N-苯磺酰基磷酰二胺酯类化合物的合成。用电生理细胞内微电极技术研究了这些化合物的结构对昆虫谷氨酸电位阻断作用的影响。结果表明:它们均能阻断果蝇幼虫神经肌肉兴奋性接点电位,但其阻断时间相差很大。阻断过程可分为3种:(1)电位逐渐被阻断;(2)电位开始有短暂的兴奋,然后被阻断;(3)电位迅速被阻断。活体实验表明:具有第2种杀虫机制的化合物杀虫效果最好。

关键词: 苯磺酰基磷酰二胺酯, 谷氨酸受体通道, 阻断时间, 阻断过程

Abstract: The synthesis of N-phenylsulfonyl phosphordaimides was reported.The effects of the structures of the compounds on the insect glutamate potentials were investigated by using electrophysiological intracellular microelectrode recording technique. The results showed that all of the compounds could block the neuromuscular junctional excitation potentials (EJP),but the blocking time had a great difference. The blocking action could be divided into three types:(1)EJP were blocked progressively;(2)EJP were blocked after a short exciting period;(3)EJP were blocked rapidly. The results of the bioassay showed that the compounds which possessed the second action mechanism had the best killing effect.

Key words: Phenylsulfonyl phosphordiamide ester, Glutamate receptor tunnel, Blocking time, Blocking process

TrendMD:

陈茹玉, 戴庆, 王惠林, 刘安西, 赵勇. N-苯磺酰基磷酰二胺酯类化合物的合成及其对昆虫谷氨酸受体通道阻断作用的研究. 高等学校化学学报, 1995, 16(8): 1215.

CHEN Ru-Yu, DAI Qing, WANG Hui-Lin, LIU An-Xi, ZHAO Yong . Synthesis of N-Phenylsulfonyl Phosphordiamides and Study on Effects of Structures on Insect Glutamate Potentials. Chem. J. Chinese Universities, 1995, 16(8): 1215.