Topiramate

For research use only.

Catalog No.S1438 Synonyms: MCN 4853, RWJ 17021

2 publications

Topiramate Chemical Structure

CAS No. 97240-79-4

Topiramate (MCN 4853, RWJ 17021) is a mutil-targeted inhibitor, including voltage-gated sodium channel and calcium channel, AMPA/kainate receptor and carbonic anhydrase, used to treat epilepsy.

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10mM (1mL in DMSO) EUR 127 In stock
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Selleck's Topiramate has been cited by 2 publications

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Biological Activity

Description Topiramate (MCN 4853, RWJ 17021) is a mutil-targeted inhibitor, including voltage-gated sodium channel and calcium channel, AMPA/kainate receptor and carbonic anhydrase, used to treat epilepsy.
Targets
sodium channel [1] Calcium Channel [1] AMPA/kainate receptor [2] Carbonic anhydrase [1]
In vitro

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. [1] 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. [2] Topiramate (TPM) suppresses voltage-sensitive Na+ channels and non-N-methyl-D-aspartate (NMDA) receptors and enhances gamma-aminobutyric acid (GABA)-mediated inhibition. [3] Topiramate selectively inhibits postsynaptic responses mediated by GluR5 kainate receptors. [4]

In vivo Topiramate (25-100 mg/kg, i.p.) produces a dose-dependent elevation in the threshold for clonic seizures induced by infusion of ATPA, a selective agonist of GluR5 kainate receptors. [4] Topiramate effectively suppresses acute seizures induced by perinatalhypoxia in a dose-related manner with a calculated ED50 of 2.1 mg/kg, i.p. [5] Topiramate (20 and 40 mg/kg i.p.) inhibits both tonic and absence-like seizures in a dose-dependent manner, whereas Phenytoin (20 mg/kg i.p.) and Zonisamide (40 mg/kg i.p.) inhibits only the tonic seizures. Topiramate inhibits sound-induced seizures in DBA/2 mice (ED50 = 8.6 mg/kg p.o.). [6]

Protocol

Solubility (25°C)

In vitro DMSO 68 mg/mL (200.37 mM)
Ethanol 68 mg/mL (200.37 mM)
Water Insoluble

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Chemical Information

Molecular Weight 339.36
Formula

C12H21NO8S

CAS No. 97240-79-4
Storage powder
in solvent
Synonyms MCN 4853, RWJ 17021
Smiles CC1(OC2COC3(C(C2O1)OC(O3)(C)C)COS(=O)(=O)N)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01229735 Completed Drug: Levetiracetam|Drug: Topiramate Epilepsy UCB Korea Co. Ltd.|UCB Pharma November 2010 Phase 4
NCT00846495 Completed Drug: topiramate|Drug: frovatriptan Migraine Clinvest|Endo Pharmaceuticals|Cady Roger M.D. August 2009 Phase 4
NCT00606411 Completed Drug: Topiramate or Placebo Sleep-Related Eating Disorder Massachusetts General Hospital January 2008 Early Phase 1
NCT01682681 Completed Drug: Topiramate Epilepsy Janssen Korea Ltd. Korea July 2007 --
NCT00394095 Completed Drug: Topiramate|Drug: Placebo Bipolar Disorder|Weight Gain University of Cincinnati|Eli Lilly and Company December 2006 Phase 4

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Carbonic Anhydrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID