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N ‐Methyl‐D‐Aspartate Receptors and Ethanol: Inhibition of Calcium Flux and Cyclic GMP Production

1989; Wiley; Volume: 52; Issue: 6 Linguagem: Inglês

10.1111/j.1471-4159.1989.tb07280.x

1471-4159

Paula L. Hoffman, Carolyn S. Rabe, Frances E. Moses, B Tabakoff,

Receptor Mechanisms and Signaling

Abstract: Measurements of calcium uptake and cyclic GMP production by cerebellar granule cells grown in primary culture demonstrated that ethanol preferentially inhibited N ‐methyl‐D‐aspartate (NMDA) receptor‐gated cation channel function. Concentrations of ethanol as low as 10 m M inhibited NMDA‐stimulated Ca 2+ uptake by >30%, and ethanol also inhibited NMDA‐stimulated (Ca 2+ ‐dependent) cyclic GMP accumulation in a similar, dose‐dependent manner. Responses to kainate were significantly less sensitive to ethanol. Studies using various concentrations of NMDA, as well as phencyclidine (PCP) and glycine, suggested that ethanol affected the “coagonist” binding site of the NMDA receptor‐channel complex, rather than the PCP recognition site.