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Zonisamide

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Chemical Structure| 68291-97-4 同义名 : CI 912;AD 810;Excegram;Exceglan;PD 110843
CAS号 : 68291-97-4
货号 : A238577
分子式 : C8H8N2O3S
纯度 : 98%
分子量 : 212.23
MDL号 : MFCD00865316
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(1177.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Sodium Channel
描述 Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug. It has shown activity in various animal models of epilepsy, and although a detailed mode of action awaits clarification it appears to block the propagation/spread of seizure discharges and to suppress the epileptogenic focus. Animal studies suggest that zonisamide possesses a more favourable therapeutic index than most other antiepileptic drugs[3]. Zonisamide may have some utility, especially as an adjunctive therapy, for the management of acute phases and weight gain in bipolar disorder and for prevention of alcohol misuse[4]. Moreover, zonisamide combination therapy was beneficial in treating motor symptoms in PD patients receiving antiparkinson drugs and was well tolerated in Japanese patients[5]. Administration of zonisamide (20 mg/kg, i.p. every 4 h × 3) following a single injection of MPTP (12.5 mg/kg, s.c.) reduced microglial Nav 1.6 and microglial activation in the striatum, as indicated by Iba-1 staining and mRNA expression of F4/80. Zonisamide may reduce neuroinflammation through the down-regulation of microglial Nav 1.6[6]. Zonisamide (adjunctive to levodopa) improved parkinsonism accompanying DLB (dementia with Lewy bodies) without worsening cognitive function or psychiatric symptoms[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.71mL

0.94mL

0.47mL

23.56mL

4.71mL

2.36mL

47.12mL

9.42mL

4.71mL
参考文献

[1]Sonsalla PK, Wong LY, et al. The antiepileptic drug zonisamide inhibits MAO-B and attenuates MPTP toxicity in mice: clinical relevance. Exp Neurol. 2010 Feb;221(2):329-34.

[2]Tanabe M, Sakaue A, et al. Centrally mediated antihyperalgesic and antiallodynic effects of zonisamide following partial nerve injury in the mouse. Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):107-14.

[3]Peters DH, Sorkin EM. Zonisamide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in epilepsy. Drugs. 1993;45(5):760‐787

[4]Buoli M, Grassi S, Ciappolino V, Serati M, Altamura AC. The Use of Zonisamide for the Treatment of Psychiatric Disorders: A Systematic Review. Clin Neuropharmacol. 2017;40(2):85‐92

[5]Matsunaga S, Kishi T, Iwata N. Combination Therapy with Zonisamide and Antiparkinson Drugs for Parkinson's Disease: A Meta-Analysis. J Alzheimers Dis. 2017;56(4):1229‐1239

[6]Hossain MM, Weig B, Reuhl K, Gearing M, Wu LJ, Richardson JR. The anti-parkinsonian drug zonisamide reduces neuroinflammation: Role of microglial Nav 1.6. Exp Neurol. 2018;308:111‐119

[7]Murata M, Odawara T, Hasegawa K, et al. Adjunct zonisamide to levodopa for DLB parkinsonism: A randomized double-blind phase 2 study. Neurology. 2018;90(8):e664‐e672