Catalog No.S1438 Synonyms: MCN 4853, RWJ 17021
Molecular Weight(MW): 339.36
Topiramate 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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Choose Selective Carbonic Anhydrase Inhibitors
|Description||Topiramate 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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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02878798||Not yet recruiting||Cryptogenic Sensory Peripheral Neuropathy||University of Utah|National Institute of Neurological Disorders and Stroke (NINDS)|NeuroNEXT Network||June 2017||Phase 2|
|NCT03018704||Not yet recruiting||Alcohol Use Disorder||VA Office of Research and Development||March 2017||Phase 4|
|NCT02945839||Not yet recruiting||Migraine||New York University School of Medicine||December 2016||--|
|NCT02273804||Recruiting||Obese Children and Adolescents||Assistance Publique - Hôpitaux de Paris||June 2016||Phase 3|
|NCT02808533||Recruiting||Schizophrenia, Schizoaffective Disorder||Centre for Addiction and Mental Health|Ontario Ministry of Health and Long Term Care||April 2016||--|
|NCT02635386||Recruiting||Polycystic Ovary Syndrome|Obesity||Womans|AstraZeneca||March 2016||Phase 3|
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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