Eliprodil is a non-competitive NR2B-NMDA (NR2B-selective N-methyl-D-aspartate) receptor antagonist(IC50=10 microM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM)[3]. Eliprodil significantly decreased the amplitude of rapid component of the delayed rectifier potassium current (I(Kr)), but slow component (I(Ks)), transient outward current (I(to)) and I(K1) were not considerably affected by the drug when measured in dog ventricular myocytes by applying the whole-cell configuration of the patch-clamp technique. Eliprodil, under normal conditions, moderately lengthens cardiac repolarisation by inhibition of I(Kr)[4]. Eliprodil administered intraperitoneally at 10 mg/kg completely prevented the loss of ChAT (choline acetyltransferase) and the loss of cells in the GCL(ganglion cell layer) [5]. A low dose of eliprodil (5 mg/kg) weakly stimulated locomotion in naive animals, whilst higher doses depressed rearing (20-40 mg/kg) and grooming (40 mg/kg), consistent with a sedative action[6]. The administration of a neuroprotective drug (eliprodil) or a thrombolytic agent (rt-PA) similarly reduce the volume of brain damage and the neurological deficit in a rat embolic stroke model[7].
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