YM90K

YM90K is a potent and selective AMPA receptor antagonist with a K_i of 84 nM. YM90K is less potent in inhibiting kainate (K_i of 2.2 μM) and NMDA (K_i of 37 μM) receptors. YM90K has neuroprotective actions^[1]. IC50 & Target:Ki: 84 nM (AMPA receptor), 2.2 μM (Kainate receptor) and 37 μM (NMDA receptor)^[1] In Vitro:YM90K co-injected with AMPA or kainate into the rat striatum protect cholinergic neurons against AMPA- or kainate-induced neurotoxicity^[1]. In Vivo:YM90K shows potent suppressive activity against audiogenic seizure in DBA/2 mice; ED₅₀ values of YM90K against tonic seizure is 2.54 mg/kg (i.p.). The duration of the anticonvulsant effects of YM90K is 30 min^[1].
In a global ischemia model, YM90K (15 mg/kg i.p.) significantly prevents the delayed neuronal death in the hippocampal CA1 region in Mongolian gerbils when administered 1 h after 5-min ischemia. The therapeutic time window for the neuroprotective effect of YM90K (30 mg/kg i.p.) is 6 h^[1].
In a focal ischemia model, YM90K (30 mg/kg i.v. bolus+10 mg/kg/h for 4 h) reduces the volume of ischemic damage in the cerebral cortex in F344 rats^[1].