PMID: 9450691Feb 5, 1998Paper

Inhibitory activity of a naturally occurring heterocyclic beta-substituted alanine, beta-(isoxazolin-5-on-4-yl)-L-alanine, on the L-glutamate/L-aspartate transporter (GLAST) expressed in Xenopus oocytes

Brain Research. Molecular Brain Research
K Kusama-EguchiK Watanabe

Abstract

Excitatory amino acid (EAA) transporters are of physiological importance in the regulation of the extracellular concentration of excitatory amino acids and the neuroexcitation in CNS. Among four identified transporters, the Na+-dependent high-affinity L-glutamate/L-aspartate transporter (GLAST) is highly expressed in glial cells. Here, we report a naturally occurring inhibitor of GLAST, derived from bovine retina, using the Xenopus oocyte expression system. Beta-(isoxazolin-5-on-4-yl)-L-alanine (TAN), an antifungal antibiotic, inhibited [14C]L-glutamate (L-Glu) transport into GLAST-expressing oocytes. TAN also served as a substrate for this transporter in voltage-clamp experiments measuring the current coupled to the EAA transport. The maximum current of TAN itself was approximately 1/3 of that of L-glutamate, and its apparent affinity was almost the same as L-Glu. In combination with L-Glu, TAN antagonized L-glutamate transport. In radioisotope experiments, the inhibitory potency of this compound against [14C]L-Glu uptake into oocytes was approximately 1/6 of that of L-(-)-threo-3-hydroxyaspartate (THA). The glucoside of TAN (TANG), occurring in seedlings of the garden pea, the lentil and some Lathyrus species, did not show an...Continue Reading

References

Nov 15, 1992·Proceedings of the National Academy of Sciences of the United States of America·T StorckW Stoffel
May 28, 1992·The New England Journal of Medicine·J D RothsteinR W Kuncl
Nov 8, 1986·Lancet·P S SpencerH H Schaumburg
Feb 1, 1995·Brain Research. Molecular Brain Research·K InoueM Tohyama
Dec 20, 1996·Environmental Toxicology and Pharmacology·K Kusama-EguchiK Watanabe

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Citations

Apr 2, 2019·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Kuniko Kusama-Eguchi
Mar 9, 2017·Natural Product Reports·Tobias BeckerWilhelm Boland

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