货号:A206081 同义名: McN 4853;RWJ 17021
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.
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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。 |
靶点 |
|
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]. |
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 | - | - |
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 |
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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
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 |