Home Metabolism Carbonic Anhydrase inhibitor Topiramate For research use only.

Topiramate

Synonyms: MCN 4853, RWJ 17021

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

Topiramate Chemical Structure

CAS: 97240-79-4

Selleck's Topiramate has been cited by 4 publications

Purity & Quality Control

Batch: Purity: >97%
97

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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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05975580 Recruiting Obesity University of California Irvine|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) August 29 2023 Phase 4
NCT04613024 Not yet recruiting Weight Loss|Pain Postoperative Stanford University July 1 2023 Early Phase 1
NCT04986631 Recruiting Obesity Childhood University of Minnesota April 4 2022 Early Phase 1
NCT03308669 Completed Healthy Eli Lilly and Company October 16 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 339.36 Formula

C12H21NO8S
CAS No. 97240-79-4 SDF Download Topiramate SDF
Smiles CC1(OC2COC3(C(C2O1)OC(O3)(C)C)COS(=O)(=O)N)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (200.37 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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