product name Topiramate
Description: Topiramate (also known as MCN 4853, RWJ 17021) is an anticonvulsant (antiepilepsy) drug and is a mutil-targeted inhibitor that has been reported to interact with various ion channel types, such as AMPA/kainate receptors, voltage-sensitive Na+ channels, NMDA receptors and GABA receptors. Topiramate in combination with phentermine was approved by the FDA in 2012 for the treatment of weight loss. Topiramate is used to treat epilepsy in children and adults, and it was originally used as an anticonvulsant. In children, it is indicated for the treatment of Lennox-Gastaut syndrome, a disorder that causes seizures and developmental delay.
References: J Pharmacol Exp Ther. 1999 Mar;288(3):960-8; Neuropharmacology. 2004 Jun;46(8):1097-104.
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)
Solubility (In vivo)
Synonyms
MCN 4853, RWJ 17021
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404542
| 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. Kinase Assay: 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. |
Related Posts
product name Topiramate
Description: Topiramate (also known as MCN 4853, RWJ 17021) is an anticonvulsant (antiepilepsy) drug and is a mutil-targeted inhibitor that has been reported to interact with various ion channel types, such as AMPA/kainate receptors, voltage-sensitive Na+ channels, NMDA receptors and GABA receptors. Topiramate in combination with phentermine was approved by the FDA in 2012 for the treatment of weight loss. Topiramate is used to treat epilepsy in children and adults, and it was originally used as an anticonvulsant. In children, it is indicated for the treatment of Lennox-Gastaut syndrome, a disorder that causes seizures and developmental delay.
References: J Pharmacol Exp Ther. 1999 Mar;288(3):960-8; Neuropharmacology. 2004 Jun;46(8):1097-104.
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)
Solubility (In vivo)
Synonyms
MCN 4853, RWJ 17021
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404542
| 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. Kinase Assay: 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. |