Chemical Name: 2,3:4,5-Bis-O-(1-methylethylidene)-β-D-fructopyranose sulfamate
Biological ActivityTopiramate is an anticonvulsant. Antagonizes GluK1 (formerly 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.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
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Topiramate attenuates voltage-gated sodium currents in rat cerebellar granule cells.
Zona et al.
Topiramate as an inhibitor of carbonic anhydrase isoenzymes.
Dodgson et al.
Topiramate selectively protects against seizures induced by ATPA, a GluR5 kainate receptor agonist.
Kaminiski et al.
Selective antagonism of GluR5 kainate-receptor-mediated synaptic currents by topir. in rat basolateral amygdala neurons.
Gryder and Rogawski
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