Topiramate

Catalog No.S1438 Synonyms: MCN 4853, RWJ 17021

For research use only.

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 Chemical Structure

CAS No. 97240-79-4

Selleck's Topiramate has been cited by 3 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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 339.36
Formula

C12H21NO8S

CAS No. 97240-79-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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
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 December 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 LLC March 2016 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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