Fanapanel (ZK200775) is a quinoxalinedione derivative and potent competitive antagonist of AMPAR for cerebrovascular-related studies.

AMPA/kainate receptor:21 nM

In rat cortical slice experiments, the inhibitory effect of Fanapanel on AMPA receptors was measured to assess its activity. The Results showed that the IC50 value for Fanapanel's inhibition of AMPA-induced currents was 21 nM, demonstrating strong neuroprotective and anticonvulsant effects [1].

In the permanent MCAO model, intravenous infusion of Fanapanel (0.1-10 mg/kg/h for 6 hours) reduced the infarct volume by 24-34%, and it remained effective even when administered 1-5 hours later (reducing infarct volume by 20-30%). In the transient MCAO model, immediate or delayed injection of Fanapanel (0.01-3 mg/kg/h) 2 hours after reperfusion reduced the infarct volume by approximately 45%. In the gerbil global cerebral ischemia model, Fanapanel protected the hippocampal CA1 region. Long-term toxicity studies (rats 6 mg/kg/h, dogs 0.2 mg/kg/h for 4 weeks) did not show renal or neurotoxicity [1].