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Topiramate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Topiramate图片
CAS NO:97240-79-4
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)339.36
FormulaC12H21NO8S
CAS No.97240-79-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 68 mg/mL (200.4 mM)
Water: < 1 mg/mL
Ethanol: 68 mg/mL (200.4 mM)
SMILESNS(OC[C@]1(OC(C)(C)O2)[C@@H]2[C@H](OC(C)(C)O3)[C@H]3CO1)(=O)=O
SynonymsTopiramate; MCN 4853; RWJ 17021; HSDB-7531; HSDB7531; Tipiramato; Topax; MCN-4853; HSDB 7531; RWJ-17021; MCN4853; RWJ17021
实验参考方法
In Vitro

In vitro activity: 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.


Cell Assay: In dissociated neurons, Topiramate inhibited the persistent fraction of Na+ current in a dose-dependent manner.

In VivoTopiramate (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.).
Animal modelMale NIH Swiss mice
Formulation & Dosage25 ~ 100 mg/kg; i.p. injection
References

J Pharmacol Exp Ther. 1999 Mar;288(3):960-8; Neuropharmacology. 2004 Jun;46(8):1097-104.