L-aspartate-beta-hydroxamate exhibits mixed agonist/antagonist activity at the glutamate metabotropic receptor in rat neonatal cerebrocortial slices.
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.
Porter
R H
RH
Department of Physiology and Pharmacology, University of Southampton, UK.
Briggs
R S
RS
Roberts
P J
PJ
D000818:Animals; D000831:Animals, Newborn; D001216:Asparagine / Q000031:analogs & derivatives* / Q000494:pharmacology; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D018691:Excitatory Amino Acid Antagonists; D066298:In Vitro Techniques; D010716:Phosphatidylinositols / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D017470:Receptors, Glutamate / Q000187:drug effects*; D013237:Stereoisomerism
D018691:Excitatory Amino Acid Antagonists; D010716:Phosphatidylinositols; D017470:Receptors, Glutamate; C024848:beta-aspartylhydroxamic acid; D001216:Asparagine