INHIBITION OF GAMMA-AMINOBUTYRATE AND GLYCINE UPTAKE INTO SYNAPTIC VESICLES

被引:46
作者
CHRISTENSEN, H
FYSKE, EM
FONNUM, F
机构
[1] Norwegian Defence Research Establishment, Division for Environmental Toxicology
来源
EUROPEAN JOURNAL OF PHARMACOLOGY-MOLECULAR PHARMACOLOGY SECTION | 1991年 / 207卷 / 01期
关键词
SYNAPTIC VESICLES; GLYCINE; GABA; VESICULAR UPTAKE;
D O I
10.1016/S0922-4106(05)80040-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The substrate specificity of vesicular GABA and glycine uptake was studied in vesicle fractions from brain and spinal cord, respectively. Glycine, beta-alanine and gamma-vinyl-GABA were competitive inhibitors of the GABA uptake by synaptic vesicles in brain. Likewise GABA and beta-alanine turned out to be competitive inhibitors of vesicular uptake of glycine in spinal cord. The apparent K(i) values were in the same range as the respective K(m) values for the transport systems. Accumulation of different amino acids were examined, and the structurally related amino acids GABA, beta-alanine and glycine were all taken up by both vesicle fractions. In the present study, we suggest that there are similarities in the vesicular transporters for GABA and glycine, and the two amino acids are probably taken up into the same vesicle population. The key factor in differentiating between GABA and glycine as transmitters in the terminals could be the synthesis and the high-affinity synaptosomal uptake.
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页码:73 / 79
页数:7
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