GYKI 52466 dihydrochloride is orally active and non-competitive kainate- and AMPA-activated currents antagonist (IC50s: 7.5 μM and 11 μM). It is inactive against NMDA or γ-aminobutyric acid responses. It is a muscle relaxant and anticonvulsant agent and h

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.

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

Osteoprotegerin is a soluble secreted member of the tumor necrosis factor receptor superfamily, inhibiting osteoclastogenesis by interrupting the signaling between stromal cells and osteoclastic progenitor cells, leading to excess accumulation of bone and cartilage.