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Talampanel(LY300164)AMPA-receptor antagonist

Talampanel(LY300164)

Catalog No. B5824
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Talampanel(LY300164)

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Chemical Properties

Cas No. 161832-65-1 SDF Download SDF
Chemical Name (R)-1-(5-(4-aminophenyl)-8-methyl-8,9-dihydro-7H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d][1,2]diazepin-7-yl)ethanone
Canonical SMILES C[C@]1([H])CC2=CC(OCO3)=C3C=C2C(C4=CC=C(N)C=C4)=NN1C(C)=O
Formula C19H19N3O3 M.Wt 337.37
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Talampanel (LY300164) is a non-competitive antagonist of AMPA-receptor [1] [2] [3].

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) is a ionotropic transmembrane receptor for glutamate, which is involved in fast synaptic transmission in the central nervous system (CNS) [1].

Talampanel (LY300164) is a non-competitive AMPA-receptor antagonist. In primary rat hippocampal cultures, LY300164 dose-dependently attenuated kainic acid (KA)-excitotoxicity with IC50 value of 4 μM [2].

In male Mongolian gerbils with bilateral carotid artery occlusion, LY300164 (10 mg/kg) orally administration reduced responses to AMPA by 68% but reduced responses to NMDA only by 9%. LY300164 (10 mg/kg) administered orally or intravenously immediately after the occlusion exhibited good protection with 24% and 20% of the neurones surviving, respectively [1]. In mice with transient focal cerebral ischemia/reperfusion, talampanel significantly reduced the infarct size by 33.1%. Also, talampanel significantly reduced the amount of TUNEL-positive cells and caspase-3 active cells [3].

References:
[1].  Lodge D, Bond A, O'Neill MJ, et al. Stereoselective effects-of 2,3-benzodiazepines in vivo: electrophysiology and neuroprotection studies. Neuropharmacology, 1996, 35(12): 1681-1688.
[2].  May PC, Robison PM, Fuson KS. Stereoselective neuroprotection by novel 2,3-benzodiazepine non-competitive AMPA antagonist against non-NMDA receptor-mediated excitotoxicity in primary rat hippocampal cultures. Neurosci Lett, 1999, 262(3): 219-221.
[3].  Denes L, Szilágyi G, Gál A, et al. Talampanel a non-competitive AMPA-antagonist attenuates caspase-3 dependent apoptosis in mouse brain after transient focal cerebral ischemia. Brain Res Bull, 2006, 70(3): 260-262.