GYKI 52466 hydrochloride

Selective, non-competitive AMPA receptor antagonist (IC₅₀ values are 10-20, approx. 450 and >50 μM for AMPA- , kainate- and NMDA-induced responses, respectively). Inactive at NMDA receptors.

GYKI 52466 shows anti-convulsant and neuroprotective actions. It also acts as a skeletal muscle relaxant. The compounds is active in vivo and its effects have been shown to last from 60 to 90 min with plasma concentrations peaking within 15min and decreasing to <5% of peak levels within 90min of i.p. injection.