- Topiramate 97240-79-4
- Topiramate 97240-79-4
Topiramate 97240-79-4
产品描述 描述 Topiramate (brand name Topamax) is an anticonvulsant drug produced by Ortho-McNeil Neurologics, a division of Johnson & Johnson. It is used to treat epilepsy in both children and adults. In children it is also indicated for treatment of Lennox-Gastaut syndrome (a disorder that causes seizures and developmental delays). It is also Food and Drug Administration (FDA) approved for, and now most frequently prescribed for, the prevention of migraines. . A combination product containing phentermine and topiramate extended-release called QSYMIA? is indicated for the management of obesity. On August 2013, an extended released formulation, marketed as Trokendi XR has been approved for the management of partial onset, tonic-clonic, and Lennox-Gastaut Syndrome seizures.
纯度 99%储存/保存方法 Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.基本信息 别名 McN 4853；RWJ 17021外观 白色粉末可溶性/溶解性 DMSO : 33.9 mg/mL (100 mM)
Ethanol : 33.9 mg/mL (100 mM)生物活性 靶点 sodium channel,Calcium Channel,AMPA/kainate receptor,Carbonic anhydraseIn vitro(体外研究) Topiramate slightly inhibits the persistent fraction of Na+ current in dissociated neurons and reduces the Na+-dependent long-lasting action potential shoulders, which can be evoked in layer V pyramidal neurons after Ca+ and K+ current blockade in neocortical slices. Topiramate at low concentrations (IC50, approximately 0.5 mM) selectively inhibits pharmacologically isolated excitatory synaptic currents mediated by kainate receptors containing the GluR5 subunit in whole-cell voltage-clamp recordings from principal neurons of the rat basolateral amygdala. Topiramate also partially depresses predominantly AMPA-receptor-mediated EPSCs, but with lower efficacy. Topiramate (TPM) suppresses voltage-sensitive Na+ channels and non-N-methyl-D-aspartate (NMDA) receptors and enhances gamma-aminobutyric acid (GABA)-mediated inhibition. Topiramate selectively inhibits postsynaptic responses mediated by GluR5 kainate receptors.In vivo(体内研究) Topiramate (25-100 mg/kg, i.p.) produces a dose-dependent elevation in the threshold for clonic seizures induced by infusion of ATPA, a selective agonist of GluR5 kainate receptors. Topiramate effectively suppresses acute seizures induced by perinatalhypoxia in a dose-related manner with a calculated ED50 of 2.1 mg/kg, i.p. Topiramate (20 and 40 mg/kg i.p.) inhibits both tonic and absence-like seizures in a dose-dependent manner, whereas Phenytoin (20 mg/kg i.p.) and Zonisamide (40 mg/kg i.p.) inhibits only the tonic seizures. Topiramate inhibits sound-induced seizures in DBA/2 mice (ED50 = 8.6 mg/kg p.o.).参考文献 参考文献 1. Nowakowska E, et al. Arzneimittelforschung. 2009;59(10):487-92.
10. Braga MF, et al. J Pharmacol Exp Ther. 2009 Aug; 330(2):558-66.
2. Coppola G, et al. Epilepsy Res. 2002 Mar;49(1):45-8.
3. Rogawski MA, et al. Ann N Y Acad Sci. 2003 Apr;985:150-62.
4. Maryanoff BE, et al. J Med Chem. 2005 Mar 24;48(6):1941-7.
研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryTopiramate 97240-79-4温馨提示：本产品仅作科研实验使用，不支持临床等研究