l-Aspartate-β-hydroxamate exhibits mixed agonist/antagonist activity at the glutamate metabotropic receptor in rat neonatal cerebrocortial slices

Porter, Richard H.P., Briggs, Roger S.J. and Roberts, Peter J. (1992) l-Aspartate-β-hydroxamate exhibits mixed agonist/antagonist activity at the glutamate metabotropic receptor in rat neonatal cerebrocortial slices. Neuroscience Letters, 144 (1-2), 87-89. (doi:10.1016/0304-3940(92)90722-J).

Record type: Article

Abstract

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

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