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)|
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|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|
|NCT04986631||Not yet recruiting||Drug: Topiramate Tablets||Obesity Childhood||University of Minnesota||December 2021||Early Phase 1|
|NCT04613024||Not yet recruiting||Drug: Topamax|Drug: Gabapentin||Weight Loss|Pain Postoperative||Stanford University||May 1 2021||Early Phase 1|
|NCT03308669||Completed||Drug: Lasmiditan|Drug: Placebo|Drug: Topiramate||Healthy||Eli Lilly and Company||October 16 2017||Phase 1|
|NCT02607891||Completed||Drug: GWP42003-P|Drug: Placebo||Epilepsy||GW Research Ltd||November 9 2016||Phase 2|
|NCT02714062||Completed||Drug: Placebo|Drug: VI-0521 Mid Dose|Drug: VI-0521 Top Dose||Pediatric Obesity|Childhood Obesity||VIVUS Inc.||March 2016||Phase 4|
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