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Inhibition by riluzole of electrophysiological responses mediated by rat kainate and NMDA receptors expressed in Xenopus oocytes
Ist Teil von
European journal of pharmacology, 1993-04, Vol.235 (2), p.283-289
Ort / Verlag
Amsterdam: Elsevier B.V
Erscheinungsjahr
1993
Link zum Volltext
Quelle
Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
Beschreibungen/Notizen
The effects of riluzole, an anticonvulsant and neuroprotective compound, on excitatory amino acid-evoked currents were studied in
Xenopus laevis oocytes injected with mRNA from rat whole brain or cortex. Responses to kainic acid were blocked by riluzole (IC
50=167
μM), as well as by the quinoxalinedione antagonists 6-cyano-7-nitroquinoxaline-2,3-dione CNQX:IC
50=0.21
μM) and 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo[f]quinoxaline (NBQX:IC
50 = 0.043
μM). Riluzole was somewhat more potent at blocking responses to N-methyl-D-aspartic acid (NMDA:IC
50 = 18.2
μM); the competitive NMDA receptor antagonist 2-amino-phosphonovaleric acid (2-APV) yielded an IC
50 of 6.1 μM in this system. The inhibition by both riluzole and 2-APV was reversible and did not appear to be use dependent, unlike that of the channel blocker MK-801 ([+]-5-methyl-10,11-dihydro-5H-dibenzo-[a,d]c cyclohepten-5,10-imine maleate). It was impossible to demonstrate an interaction of riluzole with any of the known ligand recognition sites on either the kainate or the NMDA receptor in radioligand binding studies. These results suggest a direct but non-competitive action of riluzole on ionotropic glutamate receptors.