Inhibition of L-glutamate uptake into synaptic vesicles.
The effects of different agents similar in structure to glutamate were tested for inhibition of the vesicular uptake of L-glutamate. Kainate and L-homocysteate turned out to be non-competitive inhibitors of the L-glutamate uptake. Kainate was not taken up by the vesicle fraction. The vesicular uptake of gamma-aminobutyric acid (GABA) was also inhibited by kainate and L-homocysteate. Kynurenate, on the other hand, strongly inhibited the uptake of L-glutamate, whereas the uptake of GABA was hardly affected. L-alpha-Aminoadipate and D-glutamate inhibited the uptake of L-glutamate, whereas L- and D-aspartate and L-cysteate only weakly inhibited the uptake of L-glutamate. GABA, glycine, L-serine and taurine did not inhibit the uptake of L-glutamate.
Fykse
E M
EM
Norwegian Defence Research Establishment, Division for Environmental Toxicology, Kjeller.
Iversen
E G
EG
Fonnum
F
F
D000596:Amino Acids / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000378:metabolism*; D005971:Glutamates / Q000378:metabolism* / Q000494:pharmacology; D006710:Homocysteine / Q000031:analogs & derivatives / Q000494:pharmacology; D007536:Isomerism; D007608:Kainic Acid / Q000494:pharmacology*; D007700:Kinetics; D007736:Kynurenic Acid / Q000494:pharmacology; D051381:Rats; D013572:Synaptic Vesicles / Q000187:drug effects / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D000596:Amino Acids; D005971:Glutamates; D006710:Homocysteine; C007956:homocysteic acid; D005680:gamma-Aminobutyric Acid; D007736:Kynurenic Acid; D007608:Kainic Acid