INHIBITION OF N-METHYL-D-ASPARTATE-INDUCED NORADRENALINE RELEASE BY ALCOHOLS IS RELATED TO THEIR HYDROPHOBICITY

被引:32
作者
FINK, K [1 ]
GOTHERT, M [1 ]
机构
[1] UNIV BONN,INST PHARMACOL & TOXICOL,REUTERSTR 2B,W-5300 BONN 1,GERMANY
关键词
Aliphatic alcohols; Cerebral cortex (rat); Ethanol; NMDA receptors; Noradrenaline release;
D O I
10.1016/0014-2999(90)94152-N
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In rat brain cortex slices, ethanol was three times more potent in inhibiting [3H]noradrenaline ([3H]NA) release evoked by N-methyl-D-aspartate (NMDA) than in inhibiting the release evoked by kainic acid. Methanol, 1-propanol, 1-butanol, 1-pentanol and 1-hexanol shared the inhibitory property of ethanol on NMDA-evoked [3H]NA release. The inhibitory potency of the alcohols, as expressed by their IC50 values, was correlated with their membrane/buffer partition coefficient. It is concluded that the inhibitory effect of the alcohols may be due to a hydrophobic interaction with the NMDA receptor system. © 1990.
引用
收藏
页码:225 / 229
页数:5
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