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Cat. No. Name Size Price Add Cart
KI0765Topiramate100 mg$154

Chemical Characteristic

Product NameTopiramate
SynonymsTopamax
CAS No.97240-79-4
Molecular Weight 339.36
FormulaC12H21NO8S
Chemical Structure

Biological activities

Topiramate is an anticonvulsant (antiepilepsy) drug. Topiramate interacts with various ion channel types, including AMPA/kainate receptors. In whole-cell voltage-clamp recordings from principal neurons of the rat basolateral amygdala, topiramate selectively inhibits pharmacologically isolated excitatory synaptic currents mediated by kainate receptors containing the GluR5 subunit with an IC50 of 0.5 µM.[1] Topiramate blocks kainate-evoked inward currents in cultured hippocampal neurons in vitro.[2] Topiramate The Ki values of topiramate for HCA I (human carbonic anhydrase I), HCA II, HCA IV, and HCA VI are approximately 100, 7, 10, and >100 µM, respectively. The Ki values of topiramate for RCA I (rat carbonic anhydrase I), RCA II, RCA III, RCA IV, and RCA V are approximately 180, 0.1 to 1, >100, 0.2 to 10 and 18 µM, respectively. The Ki values of topiramate for MCA II (mouse carbonic anhydrase I) and MCA IV ranges between 1 and 20 µM and are temperature-dependent.[3] In rat cerebellar granule cells in vitro, topiramate (10-1000 µM) reduces tetrodotoxin-sensitive inward voltage-gated Na+ currents in a dose-related manner with an IC50 of 48.9 µM. Topiramate also makes the steady-state inactivation curve of the current shift toward more negative values.[4] 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 receptor) in mice.[5]

Protocols

In vitro: Topiramate is dissolved in DMSO.[2]

References

[1] Gryder DS, et al. Selective antagonism of GluR5 kainate-receptor-mediated synaptic currents by topiramate in rat basolateral amygdala neurons. J Neurosci. 2003, 23(18): 7069-7074.
[2] Gibbs JW 3rd, et al. Cellular actions of topiramate: blockade of kainate-evoked inward currents in cultured hippocampal neurons. Epilepsia. 2000, 41 Suppl 1: S10-16.
[3] Dodgson SJ, et al. Topiramate as an inhibitor of carbonic anhydrase isoenzymes. Epilepsia. 2000, 41閿涘湯uppl 1閿? S35-39. 閵嗏偓閵嗏偓
[4] Zona C, et al. Topiramate attenuates voltage-gated sodium currents in rat cerebellar granule cells. Neurosci Lett. 1997, 231(3): 123-126.
[5] Kaminski RM, et al. Topiramate selectively protects against seizures induced by ATPA, a GluR5 kainate receptor agonist. Neuropharmacology. 2004, 46(8): 1097-1104. 閵嗏偓閵嗏偓

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