Topiramate是一种口服有效的磺胺衍生单糖，具有广谱抗癫痫活性。
Cas No.:97240-79-4
Sample solution is provided at 25 µL, 10mM.
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Topiramate is an orally active sulfa-derivative monosaccharide with a broad spectrum of antiepileptic activity [1]. Topiramate can increase cerebral GABA concentrations, enhancing the inhibitory GABAergic transmission by binding to allosteric GABA-A receptors, and can inhibit brain glutamate release by antagonizing AMPA kainate type of glutamate receptors [2]. Topiramate has been widely used to prevent epileptic seizures and to alleviate obesity and alcohol dependence[3].
In vitro, Topiramate (1500µM) treatment for 72 hours significantly inhibited the proliferation of SKOV3 cells and reduced the protein expressions of CDK4, CDK6, and cyclin D1[4]. Treatment with 100µg/ml Topiramate for 24 hours significantly reduced the release of IL-1β and IL-6 in primary rat microglial cells stimulated by lipopolysaccharide (LPS) [5].
In vivo, Topiramate treatment via daily subcutaneous injection at a dose of 90mg/kg/day for 8 days significantly reduced the ethanol intake of C57BL/6 mice[6]. A single intraperitoneal injection of a 100mg/kg dose of Topiramate for 2 hours significantly increased the survival rate of rats with status epilepticus and enhanced the survival rate of CA1 and CA3 pyramidal cells[7]. One hour before intracerebroventricular injection of kainic acid (KA) (0.1µg), a single intraperitoneal injection of a 100mg/kg dose of Topiramate could alleviate neuronal cell death caused by epileptic seizures in mice and reduce the p-Erk immunoreactivity in the CA3 region of the hippocampus induced by KA [8].
References:
[1] Abtahi M A, Abtahi S H, Fazel F, et al. Topiramate and the vision: a systematic review[J]. Clinical Ophthalmology, 2012: 117-131.
[2] Arnone D. Review of the use of topiramate for treatment of psychiatric disorders[J]. Annals of general psychiatry, 2005, 4(1): 5.
[3] Mirza N, Marson A G, Pirmohamed M. Effect of topiramate on acid–base balance: extent, mechanism and effects[J]. British journal of clinical pharmacology, 2009, 68(5): 655-661.
[4] Xu G, Fang Z, Clark L H, et al. Topiramate exhibits anti-tumorigenic and metastatic effects in ovarian cancer cells[J]. American journal of translational research, 2018, 10(6): 1663.
[5] Andrzejczak D, Woldan-Tambor A, Bednarska K, et al. The effects of topiramate on lipopolysaccharide (LPS)-induced proinflammatory cytokine release from primary rat microglial cell cultures[J]. Epilepsy Research, 2016, 127: 352-357.
[6] Nguyen S A, Malcolm R, Middaugh L D. Topiramate reduces ethanol consumption by C57BL/6 mice[J]. Synapse, 2007, 61(3): 150-156.
[7] Kudin A P, Debska‐Vielhaber G, Vielhaber S, et al. The mechanism of neuroprotection by topiramate in an animal model of epilepsy[J]. Epilepsia, 2004, 45(12): 1478-1487.
[8] Park H J, Kim H J, Park H J, et al. Protective effect of topiramate on kainic acid–induced cell death in mice hippocampus[J]. Epilepsia, 2008, 49(1): 163-167.
Topiramate是一种口服有效的磺胺衍生单糖，具有广谱抗癫痫活性[1]。Topiramate可增加脑内GABA浓度，通过变构结合GABA-A受体增强抑制性GABA能传递，并可拮抗AMPA红藻氨酸型谷氨酸受体，从而抑制脑内谷氨酸释放[2]。Topiramate已被广泛用于预防癫痫发作，以及减轻肥胖和酒精依赖[3]。
在体外，1500µM的Topiramate处理SKOV3细胞72小时，显著抑制了细胞增殖，并降低了CDK4、CDK6和细胞周期蛋白D1的蛋白表达[4]。100µg/ml的Topiramate处理原代大鼠小胶质细胞24小时，显著降低了脂多糖刺激的IL-1β和IL-6的释放[5]。
在体内，每日皮下注射90mg/kg/day剂量的Topiramate，连续8天，显著减少了C57BL/6小鼠的乙醇摄入量[6]。单次腹腔注射100mg/kg剂量的Topiramate，作用2小时，显著提高了癫痫持续状态大鼠的存活率，并增强了CA1和CA3锥体细胞的存活率[7]。在脑室内注射红藻氨酸前1小时，单次腹腔注射100mg/kg剂量的Topiramate，可减轻小鼠癫痫发作引起的神经元细胞死亡，并降低KA诱导的海马CA3区p-Erk免疫反应性[8]。
| Cell experiment [1]: | |
Cell lines | SKOV3 cells |
Preparation Method | SKOV3 cells were grown in DMEM/F12 medium with 10% (v/v) fetal bovine serum (FBS), antibiotic/antimycotic solution at 37°C in 5% CO2/atmosphere. Cells were seeded in 96-well plates at a density of 5×103 cells and cultured overnight. After 48h of treatment with different concentrations of Topiramate (0.1, 1, 10, 100, 1000, 1500, and 3000µM), the cell viability was measured. |
Reaction Conditions | 0.1, 1, 10, 100, 1000, 1500, and 3000µM; 72h |
Applications | Topiramate treatment significantly inhibited the cell viability of SKOV3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male ICR mice |
Preparation Method | Male ICR mice (26-30g) were housed under a 12:12h light/dark cycle with free access to food and water. Topiramate (100mg/kg) or vehicle was administered intraperitoneally (i.p.), 1h prior to KA exposure. Phosphate-buffered saline (PBS) and KA (0.1μg) were administered (i.c.v.) at the bregma (the lateral ventricle) in a 5μl volume using a 50-μl microsyringe fitted with a 26-gauge needle that was inserted to a depth of 2.4mm. The mice were transcardially perfused with PBS, then with chilled 4% paraformaldehyde in phosphate buffer (pH 7.4). After postfixation, the brains of mice were collected for analysis. |
Dosage form | 100mg/kg for once; i.p. |
Applications | Topiramate treatment significantly alleviated neuronal cell death caused by epileptic seizures in mice. |
References: | |
| Cas No. | 97240-79-4 | SDF | |
| 别名 | 托吡酯; McN 4853; RWJ 17021 | ||
| 化学名 | [(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyl-5,5a,8a,8b-tetrahydrodi[1,3]dioxolo[4,5-a:5',3'-d]pyran-3a-yl]methyl sulfamate | ||
| Canonical SMILES | CC1(OC2COC3(C(C2O1)OC(O3)(C)C)COS(=O)(=O)N)C | ||
| 分子式 | C12H21NO8S | 分子量 | 339.36 |
| 溶解度 | ≥ 16.95 mg/mL in DMSO, ≥ 24.1 mg/mL in EtOH, ≥ 2.22 mg/mL in Water with ultrasonic | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9467 mL | 14.7336 mL | 29.4672 mL |
| 5 mM | 589.3 μL | 2.9467 mL | 5.8934 mL |
| 10 mM | 294.7 μL | 1.4734 mL | 2.9467 mL |
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