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

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

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.

1S, 3R-ACPD, Cerebral cortex, Glutamate metabotropic receptor, l-Aspartate-β-hydroxamate, Neonatal rat
0304-3940
87-89
Porter, Richard H.P.
d977ae5c-0112-4ea7-8a8e-951b03a94649
Briggs, Roger S.J.
a6b65ef0-e90c-4c07-bf5b-b70130c128b3
Roberts, Peter J.
ab0ce3bd-e5a0-42a9-818c-ad502d7789f3
Porter, Richard H.P.
d977ae5c-0112-4ea7-8a8e-951b03a94649
Briggs, Roger S.J.
a6b65ef0-e90c-4c07-bf5b-b70130c128b3
Roberts, Peter J.
ab0ce3bd-e5a0-42a9-818c-ad502d7789f3

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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More information

Published date: 14 September 1992
Keywords: 1S, 3R-ACPD, Cerebral cortex, Glutamate metabotropic receptor, l-Aspartate-β-hydroxamate, Neonatal rat

Identifiers

Local EPrints ID: 479048
URI: http://eprints.soton.ac.uk/id/eprint/479048
ISSN: 0304-3940
PURE UUID: 4053764a-b4e6-485f-9e6f-c7f6cac0e5f4

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Date deposited: 19 Jul 2023 16:37
Last modified: 05 Jun 2024 18:39

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Contributors

Author: Richard H.P. Porter
Author: Roger S.J. Briggs
Author: Peter J. Roberts

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