产品名称

托吡酯(Topiramate)

一般描述

Topiramate(托吡酯) is a sulfamate-substituted monosaccharide with anticonvulsant property.

别 称

2,3:4,5-Bis-O-(1-methylethylidene)-36-D-fructo-pyranose sulfamate; McN 4853;RWJ 17021;Topamax

纯 度

≥98%(HPLC)

CAS NO.

97240-79-4

分子式

C¹²H²¹NO⁸S

分子量

339.36

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色或灰白色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

Topiramate is an anticonvulsant indicated  in the treatment of epilepsy and migraine. Topiramate enhances GABA-activated chloride channels. In addition, topiramate inhibits excitatory neurotransmission, through actions on kainate and AMPA receptors. There is evidence that topiramate has a specific effect on GluR5 kainate receptors. It  is also an inhibitor of carbonic anhydrase, particular subtypes II and IV,  but this action is weak and unlikely to be related to its anticonvulsant  actions, but may account for the bad taste and the development of renal stones seen during treatment. Its possible effect as a mood stabilizer seems to occur before anticonvulsant qualities at lower dosages. Topiramate inhibits maximal electroshock and pentylenetetrazol-induced seizures as well as partial and secundarily generalized tonic-clonic seizures in the kindling model, findings predective of a broad spectrum of antiseizure activities clinically.

Topiramate is a sulfamate-substituted monosaccharide with anticonvulsant property. Although the mechanism of action has not been fully elucidated, topiramate antagonizes kainate/AMPA subtype of the glutamate receptors, which are ligand-activated cation channels that mediate the fast component of excitatory postsynaptic currents in neurons of  the central nervous system. This antagonistic action results in stabilizing hyper-excited neural membranes, inhibiting repetitive neuronal firing, and decreasing propagation of synaptic impulses, thereby impedes seizure occurrences. In addition, this agent augments gamma-aminobenzoic acid (GABA) activity and thereby attenuating GABAnergic inhibitory transmission.

l  包装与存储

包 装

1g

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov