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/ Topiramate

托吡酯 /Topiramate {[allProObj[0].p_purity_real_show]}

货号：A206081 同义名： McN 4853;RWJ 17021 Ambeed 开学季，买赠积分，赢豪礼

Topiramate is a selective GluK1 kainate receptors (GluR5) antagonist with IC50 value of 0.46 μM which can act as a positive allosteric modulator of GABAA receptor-mediated currents, inhibit Nav channels and L-type Ca2+ channels.

Topiramate 化学结构 CAS号：97240-79-4
Topiramate 化学结构
CAS号：97240-79-4
Topiramate 3D分子结构
CAS号：97240-79-4
Topiramate 化学结构 CAS号：97240-79-4
Topiramate 3D分子结构 CAS号：97240-79-4
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Topiramate 纯度/质量文件 产品仅供科研

货号：A206081 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Carbonic Anhydrase ↓ Carbonic Anhydrase I ↓ Carbonic Anhydrase II ↓ Carbonic Anhydrase IV ↓ Carbonic Anhydrase IX ↓ Carbonic Anhydrase XII ↓ 其他靶点 纯度
Topiramate ✔ Calcium Channel {[allProObj[0].p_purity_real_show]}
Dichlorphenamide ✔ {[allProObj[0].p_purity_real_show]}
Mafenide Acetate ✔ {[allProObj[0].p_purity_real_show]}
Benzenesulphonamide ✔ {[allProObj[0].p_purity_real_show]}
Dorzolamide HCl +

Carbonic anhydrase I, Ki: 6000 nM

 		++++

Carbonic anhydrase II, Ki: 1.9 nM

 		+++

Carbonic anhydrase IV, Ki: 31 nM

 		{[allProObj[0].p_purity_real_show]}
Methazolamide ++

hCAI, Ki: 50 nM

 		+++

hCAII, Ki: 14 nM

 		++

bCAIV, Ki: 36 nM

 		{[allProObj[0].p_purity_real_show]}
Tioxolone +

CAI, Ki: 91 nM

 		{[allProObj[0].p_purity_real_show]}
U-104 ++

CAIX, Ki: 45.1 nM

 		++++

CAXII, Ki: 4.5 nM

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Topiramate 生物活性

靶点

  • Carbonic Anhydrase
描述 Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase. Topiramate (25-100 mg/kg, i.p.) produced a dose-dependent elevation in the threshold for clonic seizures induced by infusion of ATPA, a selective agonist of GluR5 kainate receptors[3]. Topiramate modulates brain activity in the prefrontal areas involved in the modulation of the subcortical circuit mediating aggression. Topiramate at higher concentrations appeared more efficient to decrease aggression in treated mice. ACC is a key brain region in which Topiramate may exert its dose-response effects on aggressive and antisocial behaviors observed in populations with psychotic disorders[4]. Topiramate produced activation in several cortical areas and in the lateral septum of resident brain mice compared with their controls. However, Topiramate induced inhibition in the medial nucleus of the amygdala, the dorsomedial nucleus of the periaqueductal gray, and especially in the anterior hypothalamic nucleus. The dose of 0.1 mM of Topiramate appeared more efficacy to treat aggression in adult mice[5].

Topiramate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00598923 Traumatic Brain Injury ... 展开 >> Epilepsy 收起 << Early Phase 1 Terminated(End of funding and ... 展开 >>low enrollment) 收起 << - -
NCT00210574 Epilepsy, Absence Phase 2 Completed - -
NCT00231556 Epilepsy Seiz... 展开 >>ures Epilepsies, Partial Epilepsy, Generalized Epilepsy, Tonic-Clonic 收起 << Phase 3 Completed - -

Topiramate 参考文献

[1]Lyseng-Williamson KA, Yang LP. Topiramate: a review of its use in the treatment of epilepsy. Drugs. 2007;67(15):2231-56.

[2]Gryder DS, Rogawski MA. Selective antagonism of GluR5 kainate-receptor-mediated synaptic currents by topiramate in rat basolateral amygdala neurons. J Neurosci. 2003 Aug 6;23(18):7069-74.

[3]Kaminski RM, Banerjee M, Rogawski MA. Topiramate selectively protects against seizures induced by ATPA, a GluR5 kainate receptor agonist. Neuropharmacology. 2004 Jun;46(8):1097-104

[4]Chaibi I, Bouchatta O, Bennis M, Ba-M'hamed S. Bidirectional effects of Topiramate on anterior cingulate cortex region related aggressive behavior. Neurosci Lett. 2020 Oct 15;737:135307

[5]Bouchatta O, Chaibi I, Baba AA, Ba-M'Hamed S, Bennis M. The effects of Topiramate on isolation-induced aggression: a behavioral and immunohistochemical study in mice. Psychopharmacology (Berl). 2020 Aug;237(8):2451-2467

Topiramate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.29mL

14.73mL

2.95mL

1.47mL

29.47mL

5.89mL

2.95mL

Topiramate 技术信息

CAS号97240-79-4
分子式C12H21NO8S
分子量 339.362
别名 McN 4853;RWJ 17021;Topax;Tipiramato;HSDB-7531;TPM
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(309.4 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 4 mg/mL(11.79 mM)，配合低频超声助溶
动物实验配方

Tags: Topiramate | 97240-79-4 | McN 4853 | RWJ 17021 | McN4853 | McN-4853 | RWJ17021 | RWJ 17021 | RWJ-17021 | Membrane Transporter/Ion Channel | Neuronal Signaling | Metabolic Enzyme/Protease | iGluR | GABA Receptor | Sodium Channel | Calcium Channel | Potassium Channel | Carbonic Anhydrase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Topiramate 纯度/质量文件 | Topiramate 亚型比较 | Topiramate 生物活性 | Topiramate 临床数据 | Topiramate 参考文献 | Topiramate 实验方案 | Topiramate 技术信息

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