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Description: Topiramate (also known as MCN 4853, RWJ 17021) is a novel, potent, anticonvulsant (antiepilepsy) drug and is a mutil-targeted inhibitor that has been reported to interact with various ion channel types, such as AMPA/kainate receptors, voltage-sensitive Na+ channels, NMDA receptors and GABA receptors.
References: J Pharmacol Exp Ther. 1999 Mar;288(3):960-8; Neuropharmacology. 2004 Jun;46(8):1097-104.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Topiramate slightly inhibits the persistent fraction of Na+ current in dissociated neurons and reduces the Na+-dependent long-lasting action potential shoulders, which can be evoked in layer V pyramidal neurons after Ca+ and K+ current blockade in neocortical slices. Topiramate at low concentrations (IC50, approximately 0.5 mM) selectively inhibits pharmacologically isolated excitatory synaptic currents mediated by kainate receptors containing the GluR5 subunit in whole-cell voltage-clamp recordings from principal neurons of the rat basolateral amygdala. Topiramate also partially depresses predominantly AMPA-receptor-mediated EPSCs, but with lower efficacy. Topiramate (TPM) suppresses voltage-sensitive Na+ channels and non-N-methyl-D-aspartate (NMDA) receptors and enhances gamma-aminobutyric acid (GABA)-mediated inhibition. Topiramate selectively inhibits postsynaptic responses mediated by GluR5 kainate receptors.
Cell Assay: In dissociated neurons, Topiramate inhibited the persistent fraction of Na+ current in a dose-dependent manner.
J Pharmacol Exp Ther. 1999 Mar;288(3):960-8; Neuropharmacology. 2004 Jun;46(8):1097-104.
Purity ≥98%
NMR