Anticonvulsant activity of 2-phthalimidoethanesulphonamides: New derivatives of taurine.

A number of 2-phthalimidoethanesulphonamides, new derivatives of the inhibitory neuromodulator taurine, were tested for their anticonvulsant activity in maximal electroshock seizure and pentetrazole seizure threshold tests in mice. Certain lower N-alkylamides showed activity, methylamide, dimethylamide and isopropylamide derivatives and the unsubstituted amide being pharmacologically most promising. Possible interferences with the intracellular uptake, release and membrane binding of taurine and GABA were assessed in an attempt to elucidate their mode of action. Since the uptake and release processes were only minimally affected, but the sodium-independent binding of GABA and/or taurine to synaptic membranes strongly reduced, the compounds studied may preferentially act as taurine or GABA receptor agonists.