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Zonisamide Sodium Channel inhibitor

Cat.No.S1445

Zonisamide (Zonegran,CI-912,AD 810) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
Zonisamide Sodium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 212.23

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Chemical Information, Storage & Stability

Molecular Weight 212.23 Formula

C8H8N2O3S

 Storage (From the date of receipt)
CAS No. 68291-97-4 Download SDF Storage of Stock Solutions

Synonyms Zonegran,CI-912,AD 810 Smiles C1=CC=C2C(=C1)C(=NO2)CS(=O)(=O)N

Solubility

In vitro
Batch:

DMSO : 42 mg/mL ( (197.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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.
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Mechanism of Action

Targets/IC50/Ki
Sodium channel [1]
In vitro

This compound 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. This compound attenuates the reduction in striatal contents of DA, its metabolite DOPAC and tyrosine hydroxylase (TH). [1] It (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.. This chemical produces antinociceptive effects against acute thermal and mechanical nociception in non-ligated mice. [2] It reduces the cortical infarction volume to 6% from 68% in vehicle-treated controls and the striatal volume to 8% from 78% in rats. This compound also reduces neuronal necrosis in 5 hippocampal regions (the dentate gyrus, CA4, CA3, CA1, and the subiculum) in rats. [3] It 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] This chemical 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]
References
  • https://pubmed.ncbi.nlm.nih.gov/12941455/
  • https://pubmed.ncbi.nlm.nih.gov/9720801/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04774250 Terminated
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
Partial Onset Seizures
Eisai Inc.
 March 2012 --
NCT01283256 Completed
Partial Generalized and Combined Seizures
Eisai Inc.
 January 2011 --
NCT01765608 Completed
Sleep Apnea|Obstructive Sleep Apnea|Obesity
Göteborg University|Eisai Inc.
 March 2010 Phase 2
NCT00203450 Completed
Obesity
Tuscaloosa Research & Education Advancement Corporation|Eisai Inc.
 May 2003 Phase 4

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