GYKI-53405

GYKI-53405 is a racemic small molecule from the 2,3-benzodiazepine class that acts as a **noncompetitive antagonist of the AMPA subtype of glutamate receptors**, with additional but much weaker activity at kainate receptors[3][6][8][10]. It binds allosterically, not at the classical orthosteric glutamate binding site, and inhibits AMPA receptor-mediated excitatory transmission in the central nervous system[6][8]. This compound has been studied as an **anticonvulsant** and neuroprotective agent, particularly in preclinical seizure and epilepsy models, and exhibits strong anticonvulsant effects in rodents[3][4]. It is the racemate of talampanel, an AMPA antagonist developed for epilepsy, gliomas, and ALS. GYKI-53405 has been investigated as a research tool and potential drug, but as of current data, it has not advanced beyond preclinical or early-stage clinical studies[3][4][10].

Other names

7-acetyl-5-(4-aminophenyl)-8-methyl-8,9-dihydro-7H-1,3-dioxolo[4,5-b][2,3]benzodiazepineracemate of talampanel