GYKI 52466 (hydrochloride)

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). 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, Cay-18511) 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.Formal Name: 4-(8-methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine, monohydrochloride. CAS Number: 192065-56-8. Molecular Formula: C17H15N3O2 . HCl. Formula Weight: 329.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Methanol: 1 mg/ml. SMILES: CC1=NN=C(C2=CC=C(N)C=C2)C3=C(C=C4OCOC4=C3)C1.Cl. InChi Code: InChI=1S/C17H15N3O2.ClH/c1-10-6-12-7-15-16(22-9-21-15)8-14(12)17(20-19-10)11-2-4-13(18)5-3-11,/h2-5,7-8H,6,9,18H2,1H3,1H. InChi Key: RUBSCPARMVJNKX-UHFFFAOYSA-N.