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Talampanel is an allosteric AMPA receptor antagonist (IC50 = 2.5 µM in cerebellar Purkinje neurons using voltage-clamp electrophysiology).1 It reduces the firing rate of spinal neurons in rats by 68% when administered at a dose of 10 mg/kg following AMPA administration.2 It is protective against seizures in mouse models of epilepsy including maximum electroshock (MES; ED50 = 8.6 mg/kg) and 4-aminopyridine models (Item No. 18511; ED50 = 8.4 mg/kg). It also potentiates the effects of diazepam in MES- and metrazole-induced seizure models when administered at a dose of 2 mg/kg.3 Talampanel is neuroprotective, reducing lesion size in rat and mouse models of focal ischemia.
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1. Activity of 2,3-
2. Stereoselective effects-
3. Talampanel. Neurotherapeutics 4(1), 126-129 (2007).