| 10779701 |
Kovacs I, Szarics E, Skuban N, Kardos J: Deramciclane inhibits N-methyl-D-aspartate receptor function. . Brain Res Bull. 2000 May 1;52(1):39-44.
Effects of the novel anxiolytic drug deramciclane on excitatory amino acid release and transmembrane Ca (2+) ion flux processes were compared in rat cerebrocortical homogenates containing resealed plasmalemma fragments and nerve endings. Deramciclane (10 microM) significantly inhibited [(3) H] D-aspartate release and transmembrane Ca (2+) flux to N-methyl-D-aspartate in the absence of Mg (2+). By contrast, inhibition of [(3) H] D-aspartate release and transmembrane Ca (2+) flux evoked by 0.1 mM (S)-alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate in the presence of Mg (2+) and 10 microM cyclothiazide by 10 microM deramciclane was not significant. In the presence of N-methyl-D-aspartate receptor antagonists, deramciclane (10 microM) did not inhibit [(3) H] D-aspartate release to N-methyl-D-aspartate. These results suggest an involvement of the inhibition of a presynaptic N-methyl-D-aspartate receptor in the anxiolytic properties of deramciclane. |
2(0,0,0,2) |