gyki 52466 dihydrochloride

GYKI 52466 dihydrochloride (GYKI 52466 2HCl) 是一种具有良好的血脑屏障通透性、口服活性和选择性的 AMPA Kainate 受体拮抗剂，具有抗惊厥活性，可用于研究帕金森和癫痫等神经系统疾病。

GYKI-52466 is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >50 μM for AMPA-, kainate- and NMDA-induced responses, respectively) used as a Skeletal muscle relaxant, orally active anticonvulsant, neuroprotective and

GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP) when administered at doses of 25 and 50 mg/kg. GYKI 52466 (30 mg/kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.