Description: GluR5 antagonist; inhibits carbonic anhydrase (CA) II and IV
Alternative Names: Topamax
Chemical Name: 2,3:4,5-Bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Anticonvulsant. Antagonizes GluR5 kainate receptors (IC50 = 0.46 μM), acts as a positive allosteric modulator of GABAA receptor-mediated currents, inhibits Nav channels (IC50 = 48.9 μM) and inhibits L-type Ca2+ channels. Also inhibits carbonic anhydrase (CA) (Ki values are 0.1 and 0.2 μM at rat CA II and CA IV respectively), which lowers intracellular neuronal pH.
Compound Libraries
Topiramate is also offered as part of the
Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
33.94
100
ethanol
33.94
100
Preparing Stock Solutions
The following data is based on the product molecular weight 339.36. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.95 mL
14.73 mL
29.47 mL
5 mM
0.59 mL
2.95 mL
5.89 mL
10 mM
0.29 mL
1.47 mL
2.95 mL
50 mM
0.06 mL
0.29 mL
0.59 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Zonaet al (1997) Topiramate attenuates voltage-gated sodium currents in rat cerebellar granule cells. Neurosci.Lett. 231 123 PMID: 9300637
Dodgsonet al (2000) Topiramate as an inhibitor of carbonic anhydrase isoenzymes. Epilepsia 41 S35 PMID: 10768298
Gryder and Rogawski
(2003) Selective antagonism of GluR5 kainate-receptor-mediated synaptic currents by topiramate in rat basolateral amygdala neurons. J.Neurosci. 23 7069 PMID: 12904467
Kaminiskiet al (2004) Topiramate selectively protects against seizures induced by ATPA, a GluR5 kainate receptor agonist. Neuropharmacology 46 1097 PMID: 15111016