In vivo pharmacology of BIIR 561 CL, a novel combined antagonist of AMPA receptors and voltage-dependent Na~+ channels

摘要

Glutamate receptors of theα-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid(AMPA) subtype and voltage-gated Na~+ channels are associated with diseases of the central nervous system characterized by neuronal over-excitation as in epilepsy or cerebral ischaeia. In animal models, AMPA receptor antagonists and Na~+ channel blockers provide protection in these conditions. Dimethyl-{2-[2-(3-phenyl-[1,2,4]-oadiazol-5-yl)-phenoxyl]-ethyl}-amine hydrochloride(BIIR 561 CL)combines both, AMPA receptor-and Na~+ channel blocking properties in one molecule.