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Topiramate

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Chemical Structure| 97240-79-4 同义名 : McN 4853;RWJ 17021;Topax;Tipiramato;HSDB-7531;TPM
CAS号 : 97240-79-4
货号 : A206081
分子式 : C12H21NO8S
纯度 : 98%
分子量 : 339.362
MDL号 : MFCD00865320
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：
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].
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 - -
实验方案
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
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