Ralitoline is thiazolidinylidene derivative patented by Goedecke A.-G. as an anticonvulsant. In preclinical models, ralitoline blocks 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. Ralitoline inhibit the binding of tritiated batrachotoxinin A 20-alpha-benzoate ([3H]BTX-b) to rat brain synaptosomes. In healthy volunteers with single and multiple doses (50-200 mg). ralitoline is well absorbed by oral ingestion, with peak plasma concentrations occurring approximately 2-3 hr postdose. Approximately 2 weeks of administration of ralitoline had no effect on the steady-state kinetics of phenytoin or phenobarbitone in healthy volunteers.