Novel bisbenzamidines and bisbenzimidazolines as noncompetitive NMDA receptor antagonists.
Novel bisbenzamidines and bisbenzimidazolines as noncompetitive NMDA receptor antagonists.
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新型双苯甲脒和双苯并咪唑啉作为非竞争性 NMDA 受体拮抗剂。
DOI：
10.1016/s0960-894x(99)00184-5
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发表时间：
1999
影响因子：
2.7
通讯作者：
Donkor,IO
中科院分区：
文献类型：
--
作者：
Tao,B;Huang,TL;Sharma,TA;Reynolds,IJ;Donkor,IO
研究了一系列连接芳香族基团的新型双苯甲酰胺类和双苯并咪唑类化合物的NMDA受体拮抗剂活性。这些化合物的IC50值从1.2IC50M到200NMDAM。在所有的五胺类化合物中，以高哌嗪环为中心的双苯并咪胺被发现是最有效的μ受体拮抗剂。
A series of novel bisbenzamidines and bisbenzimidazolines with different linker connecting the aromatic groups was tested in vitro for NMDA receptor antagonist activity. IC50values for these compounds ranged from 1.2 to >200 μM. The bisbenzamidine with a homopiperazine ring as the central linker was found to be the most potent NMDA receptor antagonist among all the pentamidine analogues tested so far.