| CAS NO: | 97240-79-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| 10g | 电议 |
| Molecular Weight (MW) | 339.36 |
|---|---|
| Formula | C12H21NO8S |
| CAS No. | 97240-79-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 68 mg/mL (200.4 mM) |
| Water: < 1 mg/mL | |
| Ethanol: 68 mg/mL (200.4 mM) | |
| SMILES | NS(OC[C@]1(OC(C)(C)O2)[C@@H]2[C@H](OC(C)(C)O3)[C@H]3CO1)(=O)=O |
| Synonyms | Topiramate; MCN 4853; RWJ 17021; HSDB-7531; HSDB7531; Tipiramato; Topax; MCN-4853; HSDB 7531; RWJ-17021; MCN4853; RWJ17021 |
| In Vitro | In vitro activity: 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. Cell Assay: In dissociated neurons, Topiramate inhibited the persistent fraction of Na+ current in a dose-dependent manner. |
|---|---|
| In Vivo | 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.). |
| Animal model | Male NIH Swiss mice |
| Formulation & Dosage | 25 ~ 100 mg/kg; i.p. injection |
| References | J Pharmacol Exp Ther. 1999 Mar;288(3):960-8; Neuropharmacology. 2004 Jun;46(8):1097-104. |
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