Bioactivity | YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions[1]. |
Target | Ki: 84 nM (AMPA receptor), 2.2 μM (Kainate receptor) and 37 μM (NMDA receptor) |
Invitro | 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]. |
Name | YM90K |
CAS | 154164-30-4 |
Formula | C11H8ClN5O4 |
Molar Mass | 309.67 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. M Shimizu-Sasamata, et al. YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist. J Pharmacol Exp Ther. 1996 Jan;276(1):84-92. |