Home Transmembrane Transporters Sodium Channel inhibitor Zonisamide

Zonisamide

Catalog No.S1445 Synonyms: CI-912

For research use only.

Zonisamide (CI-912) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.

Zonisamide Chemical Structure

CAS No. 68291-97-4

Selleck's Zonisamide has been cited by 1 Publication

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Biological Activity

Description Zonisamide (CI-912) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
Targets
Sodium channel [1]
In vitro

Zonisamide inhibits monoamine oxidase B (MAO-B) activity in vitro with an IC(50) of 25 μM. [1]
In vivo Zonisamide modifies dopamine (DA) activity, provides protection in ischemia mice models and influences antioxidant systems. Zonisamide attenuates the reduction in striatal contents of DA, its metabolite DOPAC and tyrosine hydroxylase (TH). [1] Zonisamide (10 and 30 mg/kg) produces antihyperalgesic and antiallodynic effects in a dose-dependent manner, these effects are manifested by elevation of the withdrawal threshold in response to a thermal (plantar test) or mechanical (von Frey) stimulus, respectively.. Zonisamide produces antinociceptive effects against acute thermal and mechanical nociception in non-ligated mice. [2] Zonisamide reduces the cortical infarction volume to 6% from 68% in vehicle-treated controls and the striatal volume to 8% from 78% in rats. Zonisamide also reduces neuronal necrosis in 5 hippocampal regions (the dentate gyrus, CA4, CA3, CA1, and the subiculum) in rats. [3] Zonisamide causes increase in the quantity of EAAC-1 protein in hippocampus and cortex and down regulation of the GABA transporter GAT-1 in rats with hippocampal seizures. [4] Zonisamide inhibits both the 50 mM KCl-evoked hippocampal glutamate release (AUC for 60 min) from 9.2 mM to 5.8 mM in urethane-anaesthetized rats, as well as the stimulatory effects of Ca2+ on KCl-evoked hippocampal glutamate release. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

 DMSO 42 mg/mL
(197.89 mM)
Ethanol 5 mg/mL
(23.55 mM)
Water 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.

Chemical Information

Molecular Weight 212.23
Formula

C8H8N2O3S
CAS No. 68291-97-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C(=C1)C(=NO2)CS(=O)(=O)N

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04774250 Enrolling by invitation Drug: Zonisamide 100Mg Cap|Drug: Placebo Hearing Loss Noise-Induced Washington University School of Medicine|United States Department of Defense|University of Texas|Gateway Biotechnology Inc. November 10 2021 Phase 2
NCT01830868 Completed Drug: Zonisamide tablets Partial Onset Seizures Eisai Inc. March 2012 --
NCT01283256 Completed Drug: zonisamide Partial Generalized and Combined Seizures Eisai Inc. January 2011 --
NCT01765608 Completed Drug: Zonisamide|Drug: Placebo|Device: nCPAP Sleep Apnea|Obstructive Sleep Apnea|Obesity Göteborg University|Eisai Inc. March 2010 Phase 2
NCT00203450 Completed Drug: Zonegran|Drug: Placebo Obesity Tuscaloosa Research & Education Advancement Corporation|Eisai Inc. May 2003 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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