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Título

Effect of 1-aminocyclopropanecarboxylic acid on N-methyl-D-aspartate-stimulated [3H]-noradrenaline release in rat hippocampal synaptosomes

AutorClos, M. V.; García Sanz, A.; Trullás Oliva, Ramón; Badía, A.
Palabras claveACPC
NMDA receptor
Glycine
Hippocampus
Noradrenaline release
Fecha de publicaciónjun-1996
EditorNational Institutes of Health (U.S.). PubMed Central
CitaciónBritish Journal of Pharmacology 118(4): 901-904 (1996)
ResumenThe effect of 1-aminocyclopropanecarboxylic acid (ACPC), a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor complex that exhibits neuroprotective, anxiolytic and antidepressant-like actions, was investigated in a functional assay for presynaptic NMDA receptors.
NMDA (100 microM) produced a 36% increase of tritium efflux above basal efflux in rat hippocampal synaptosomes preincubated with [3H]-noradrenaline ([3H]-NA), reflecting a release of tritiated noradrenaline. This effect was prevented by 10 microM 7-chlorokynurenic acid, an antagonist of the glycine site of the NMDA receptor.
Glycine enhanced the effect of NMDA with Emax and EC50 values of 84 +/- 11% and 1.82 +/- 0.04 microM, respectively. ACPC potentiated the effect of NMDA on tritium overflow with a lower EC50 (43 +/- 6 nM) and a lower maximal effect (Emax = 40 +/- 9%) than glycine. Furthermore, ACPC (0.1 microM) shifted the EC50 of glycine from 1.82 microM to > or = 3 mM.
These results show that ACPC can reduce the potentiation by glycine of NMDA-evoked [3H]-NA release and hence, may act as an antagonist at the glycine site of presynaptic hippocampal NMDA receptors when the concentration of glycine is high.
Descripción4 pages, 3 figures.-- PMID: 8799560 [PubMed].-- PMCID: PMC1909537.
Versión del editorhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC1909537
URIhttp://hdl.handle.net/10261/26535
ISSN0007-1188 (Print)
1476-5381 (Online)
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