Effects of the anticonvulsant taurine derivative, taltrimide, on membrane transport and binding of GABA and taurine in the mouse cerebrum.
The effects of a new anticonvulsive derivative of taurine, taltrimide (2-phthalimido-ethanesulphon-N-isopropylamide), and its metabolites on the release, uptake and binding of gamma-aminobutyric acid (GABA) and taurine, were studied in the cerebrum of the mouse. The potassium-stimulated release of taurine from slices of cerebral cortex was inhibited in vitro by taltrimide and its dealkylated metabolite, whereas the stimulated release of GABA was significantly enhanced by both drugs. The uptake of taurine and GABA were not markedly affected. Both taltrimide and its dealkylated metabolite strongly inhibited the sodium-independent binding of taurine to synaptic membranes of brain, the effects on the binding of GABA being less pronounced. The actions on synaptic binding of taurine and on depolarization-stimulated release of GABA may be of significance for their anticonvulsant properties.
D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D002462:Cell Membrane / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D008564:Membrane Potentials; D051379:Mice; D010797:Phthalimides / Q000494:pharmacology*; D011963:Receptors, GABA-A / Q000378:metabolism; D013574:Synaptosomes / Q000378:metabolism; D013654:Taurine / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D000927:Anticonvulsants; D010797:Phthalimides; D011963:Receptors, GABA-A; D013654:Taurine; C051947:2-phthalimidoethanesulfonamide; D005680:gamma-Aminobutyric Acid; C046932:taltrimide