Novel anticonvulsant taurine derivatives.
A number of novel taurine derivatives were tested for their anticonvulsant activity in maximal electroshock seizure and pentetrazole seizure threshold tests in mice. Certain piperidino, benzamido, phthalimido, and phenylsuccinylimido derivatives of taurinamide were effective, the phthalimido derivatives appearing pharmacologically most promising. Possible interferences with the intracellular release, uptake, and membrane binding of taurine and GABA were assessed in an attempt to elucidate the mode of action of the active compounds. Since the uptake and release processes of taurine and GABA were only slightly affected, but the sodium-independent binding of GABA and/or taurine to synaptic membranes strongly inhibited, the test compounds may preferentially act as taurine or GABA receptor agonists.
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001693:Biological Transport, Active / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D013570:Synaptic Membranes / Q000378:metabolism; D013654:Taurine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D000927:Anticonvulsants; D013654:Taurine; D005680:gamma-Aminobutyric Acid