Talampanel

Talampanel is an allosteric AMPA receptor antagonist (IC50 = 2.5 µM in cerebellar Purkinje neurons using voltage-clamp electrophysiology). It reduces the firing rate of spinal neurons in rats by 68% when administered at a dose of 10 mg/kg following AMPA administration. It is protective against seizures in mouse models of epilepsy including maximum electroshock (MES, ED50 = 8.6 mg/kg) and 4-aminopyridine models (Cay-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. Talampanel is neuroprotective, reducing lesion size in rat and mouse models of focal ischemia.Formal Name: (8R)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine. CAS Number: 161832-65-1. Synonyms: GYKI 53773, LY 300164. Molecular Formula: C19H19N3O3. Formula Weight: 337.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.1 mg/ml, DMSO: 10 mg/ml. lambdamax: 238, 329 nm. SMILES: NC(C=C1)=CC=C1C2=NN(C(C)=O)[C@H](C)CC3=C2C=C(OCO4)C4=C3. InChi Code: InChI=1S/C19H19N3O3/c1-11-7-14-8-17-18(25-10-24-17)9-16(14)19(21-22(11)12(2)23)13-3-5-15(20)6-4-13/h3-6,8-9,11H,7,10,20H2,1-2H3/t11-/m1/s1. InChi Key: JACAAXNEHGBPOQ-LLVKDONJSA-N.