GYKI 52466 hydrochloride is a non-competitive AMPA and kainate receptor antagonist. It blocks GluK3 homomeric receptors with an IC50 of 63 μM and GluK2b(R)/GluK3 heteroreceptors with an IC50 of 32 μM at high concentrations. GYKI 52466 has been reported to prevent the excitotoxic action of high extracellular glutamate levels due to its potent non-competitive AMPA receptor antagonistic effect. It has been demonstrated histologically that GYKI 52466 has neuroprotective actions in experimental models of global and focal cerebral ischaemia. The compound was widely investigated in experimental seizure models, where it provided effective protection against convulsions evoked by chemical agents such as AMPA or kainate, electroshock and audiogenic stimulation.
产品描述
An Antagonist of AMPA and Kainate Receptors
产品形式
GYKI 52466 hydrochloride is a non-competitive AMPA and kainate receptor antagonist. It blocks GluK3 homomeric receptors with an IC50 of 63 μM and GluK2b(R)/GluK3 heteroreceptors with an IC50 of 32 μM at high concentrations. GYKI 52466 has been reported to prevent the excitotoxic action of high extracellular glutamate levels due to its potent non-competitive AMPA receptor antagonistic effect. It has been demonstrated histologically that GYKI 52466 has neuroprotective actions in experimental models of global and focal cerebral ischaemia. The compound was widely investigated in experimental seizure models, where it provided effective protection against convulsions evoked by chemical agents such as AMPA or kainate, electroshock and audiogenic stimulation.