Topiramate

製品コードS1438 バッチS143805

印刷

化学情報

Chemical Structure Synonyms MCN 4853, RWJ 17021 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H21NO8S
分子量 339.36 CAS No. 97240-79-4
Solubility (25°C)* 体外 DMSO 68 mg/mL (200.37 mM)
Ethanol 68 mg/mL (200.37 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Topiramate (MCN 4853、RWJ 17021) は、てんかん治療に用いられる、電位依存性ナトリウムチャネル、カルシウムチャネル、AMPA/カイニン酸受容体、Carbonic Anhydraseなど、複数の標的を阻害する薬剤です。
in vitro 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. This compound 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. It also partially depresses predominantly AMPA-receptor-mediated EPSCs, but with lower efficacy. This chemical suppresses voltage-sensitive Na+ channels and non-N-methyl-D-aspartate (NMDA) receptors and enhances gamma-aminobutyric acid (GABA)-mediated inhibition. It selectively inhibits postsynaptic responses mediated by GluR5 kainate receptors.
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. This compound effectively suppresses acute seizures induced by perinatalhypoxia in a dose-related manner with a calculated ED50 of 2.1 mg/kg, i.p. It (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. This chemical inhibits sound-induced seizures in DBA/2 mice (ED50 = 8.6 mg/kg p.o.).

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/10027832/
  • https://pubmed.ncbi.nlm.nih.gov/12904467/
  • https://pubmed.ncbi.nlm.nih.gov/9757028/
  • https://pubmed.ncbi.nlm.nih.gov/15111016/
  • https://pubmed.ncbi.nlm.nih.gov/11558793/
  • https://pubmed.ncbi.nlm.nih.gov/8206119/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Neural signature of chronic migraine mice model and related photophobia in the primary visual cortex [ J Headache Pain, 2025, 26(1):182] PubMed: 40796816
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Cancer genes disfavoring T cell immunity identified via integrated systems approach [ Cell Rep, 2022, 40(5):111153] PubMed: 35926468
A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697] PubMed: 33517273
The anticonvulsant zonisamide positively modulates recombinant and native glycine receptors at clinically relevant concentrations [ Neuropharmacology, 2020, 182:108371] PubMed: 33122032
Effects of systemic inhibitors of acid-sensing ion channels 1 (ASIC1) against acute and chronic mechanical allodynia in a rodent model of migraine. [ Br J Pharmacol, 2018, 175(21):4154-4166] PubMed: 30079481

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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