For research use only.
Catalog No.S1438 Synonyms: MCN 4853, RWJ 17021
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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|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.|
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. 
|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.  Topiramate effectively suppresses acute seizures induced by perinatalhypoxia in a dose-related manner with a calculated ED50 of 2.1 mg/kg, i.p.  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.). |
-  Taverna S, et al. J Pharmacol Exp Ther, 1999, 288(3), 960-968.
-  Gryder DS, et al. J Neurosci, 2003, 23(18), 7069-7074.
-  Yang Y, et al. Brain Res, 1998, 804(2), 169-176.
|In vitro||DMSO||68 mg/mL (200.37 mM)|
|Ethanol||68 mg/mL (200.37 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||MCN 4853, RWJ 17021|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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