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/ Topiramate/托吡酯

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

货号：A206081 同义名： McN 4853; RWJ 17021

Topiramate是一种选择性的 GluK1 卡那酸受体（GluR5）拮抗剂，IC50 为 0.46 μM，具有抗癫痫活性，通过多种途径如 GABA 调节、钠钙通道抑制发挥作用。

Topiramate/托吡酯 化学结构 CAS号：97240-79-4
Topiramate/托吡酯 化学结构
CAS号：97240-79-4
Topiramate/托吡酯 3D分子结构
CAS号：97240-79-4
Topiramate/托吡酯 化学结构 CAS号：97240-79-4
Topiramate/托吡酯 3D分子结构 CAS号：97240-79-4
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Topiramate/托吡酯 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:

全球学术期刊中引用的产品

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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 98%
Dichlorphenamide ✔ 98%
Mafenide Acetate ✔ 98%
Benzenesulphonamide ✔ 98%
Dorzolamide HCl +

Carbonic anhydrase I, Ki: 6000 nM

 		++++

Carbonic anhydrase II, Ki: 1.9 nM

 		+++

Carbonic anhydrase IV, Ki: 31 nM

 		98%
Methazolamide ++

hCAI, Ki: 50 nM

 		+++

hCAII, Ki: 14 nM

 		++

bCAIV, Ki: 36 nM

 		98%
Tioxolone +

CAI, Ki: 91 nM

 		98%
U-104 ++

CAIX, Ki: 45.1 nM

 		++++

CAXII, Ki: 4.5 nM

 		98%
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/托吡酯 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/托吡酯 细胞实验

Cell Line
Concentration Treated Time Description References
Mouse cortical layer II/III pyramidal neurons 50 μmol/L 10 minutes To evaluate the effect of SAS on eIPSCs, results showed that SAS reversibly decreased eIPSC amplitude and prolonged the τslow decay kinetics Epilepsia. 2019 Jul;60(7):1365-1377.
C2C12 myotubes 1 or 100 μM 45 minutes To assess the effect of topiramate on glucose uptake and insulin signaling. Results showed that topiramate did not affect basal or insulin-stimulated glucose uptake. Br J Pharmacol. 2013 Oct;170(4):908-18.

Topiramate/托吡酯 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Wild-type and familial hemiplegic migraine type 1 knock-in mice Orogastric gavage 80 mg/kg/d Once daily for 7 weeks Chronic topiramate treatment reduced susceptibility to KCl- or electrical stimulation-induced spreading depressions as well as ischemic depolarizations, and improved tissue and neurological outcomes Stroke. 2015 Jan;46(1):229-36
DBA/2 mice High impulsivity mouse model Oral 12.5, 25, 50 mg/kg Acute administration: single dose 60 min before testing; Chronic administration: twice daily for 27 days Evaluate the effects of topiramate on impulsive behaviors. Acute administration reduced motor impulsivity, chronic administration reduced cognitive impulsivity. Br J Pharmacol. 2012 Sep;167(1):183-95
Mice No specific model mentioned Intraperitoneal injection 0.3, 1, 3, 10, 30, 100 mg/kg Twice daily for 5 days Investigate the effect of topiramate on glutamine synthetase activity in mouse brain. Single doses had no effect, but repeated administration dose-dependently reduced enzyme activity. Br J Pharmacol. 1999 Apr;126(7):1634-8
Rats ISDN-induced acute and chronic migraine model Intravenous injection 30 mg/kg Single injection Topiramate reversed ISDN-induced chronic mechanical allodynia, with effects comparable to those of mambalgin-1 and amiloride Br J Pharmacol. 2018 Nov;175(21):4154-4166
C57Bl/6J mice High-fat diet-induced insulin resistance model Oral (mixed in high-fat diet) 0.12% (w/w) 6 weeks continuously To assess the effect of topiramate on insulin sensitivity. Results showed that topiramate improved insulin sensitivity and increased glucose uptake in heart, skeletal muscle, and adipose tissue. Br J Pharmacol. 2013 Oct;170(4):908-18.
C57BL/6J mice Cisplatin or oxaliplatin-induced neuropathy model Intraperitoneal injection 50 mg/kg Single dose, assessed 24 hours after neuropathy induction To evaluate the analgesic effects of topiramate on cisplatin or oxaliplatin-induced neuropathy. Results showed that topiramate lacked significant anti-allodynic effects in both models. Neuro Oncol. 2014 Oct;16(10):1324-32

Topiramate/托吡酯 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/托吡酯 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/托吡酯 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/托吡酯 技术信息

CAS号97240-79-4
分子式C12H21NO8S
分子量 339.36
SMILES Code CC1(O[C@H]([C@@H](CO[C@@]2(COS(=O)(N)=O)O3)O1)[C@@H]2OC3(C)C)C
MDL No. MFCD00865320
别名 McN 4853; RWJ 17021; Topax; Tipiramato; HSDB-7531; TPM
运输蓝冰
InChI Key KJADKKWYZYXHBB-XBWDGYHZSA-N
Pubchem ID 5284627
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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/托吡酯 纯度/质量文件 | Topiramate/托吡酯 亚型比较 | Topiramate/托吡酯 生物活性 | Topiramate/托吡酯 临床数据 | Topiramate/托吡酯 参考文献 | Topiramate/托吡酯 实验方案 | Topiramate/托吡酯 技术信息

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