Delving into the Latest Updates on CI-953 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target-

Mechanism-

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Epilepsy

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

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Structure

Molecular FormulaC13H12ClN3O

InChIKeyZSBWDKCIIZYQIR-UHFFFAOYSA-N

CAS Registry97627-24-2

Ralitoline and CI-953 are anticonvulsant compounds active in both maximal electroshock and kindling models of seizures with rodents. CI-953 (IC50 = 5 microM) and ralitoline (IC50 = 2 microM) both blocked sustained repetitive firing of sodium action potentials with effects on firing activity triggered by spontaneous excitatory postsynaptic potentials at higher concentrations. No effects on iontophoretic GABA and glutamate responses were noted. Both compounds inhibited the binding of tritiated batrachotoxinin A 20-alpha-benzoate ([3H]BTX-b) to rat brain synaptosomes with apparent Kd values of 29 microM (CI-953) and 25 microM (ralitoline). Our results suggest that effects on voltage-dependent sodium channels may underlie the anticonvulsant action of these compounds.

100 Deals associated with CI-953

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