L-aspartate-beta-hydroxamate exhibits mixed agonist/antagonist activity at the glutamate metabotropic receptor in rat neonatal cerebrocortial slices

Neurosci Lett. 1992 Sep 14;144(1-2):87-9. doi: 10.1016/0304-3940(92)90722-j.

Abstract

L-aspartate-beta-hydroxamate, a glutamate uptake inhibitor, was investigated for activity at a glutamate metabotropic receptor (mGluR) in neonatal rat cerebral cortical slices. Stimulation of phosphatidylinositol hydrolysis by 100 microM (1S,3R)-ACPD was inhibited only very weakly, to a maximal extent of 28%, L-aspartate-beta-hydroxamate did however exhibit agonist activity (EC50 = 760 microM) and, although much less potent than (1S,3R)-ACPD (EC50 = 20 microM), its efficacy was approximately 70% of the latter. These results indicate that, at least in this preparation, offspartate-beta-hydroxamate is of little value as an antagonist at the mGluR receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Animals, Newborn
  • Asparagine / analogs & derivatives*
  • Asparagine / pharmacology
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism*
  • Excitatory Amino Acid Antagonists
  • In Vitro Techniques
  • Phosphatidylinositols / pharmacology
  • Rats
  • Rats, Wistar
  • Receptors, Glutamate / drug effects*
  • Stereoisomerism

Substances

  • Excitatory Amino Acid Antagonists
  • Phosphatidylinositols
  • Receptors, Glutamate
  • beta-aspartylhydroxamic acid
  • Asparagine