Showing papers on "Loreclezole published in 1991"
TL;DR: The efficacy and safety of higher loreclezole plasma concentrations were studied in a long-term follow-up trial, the results of which are presented in the following article.
19 citations
TL;DR: The effect and safety of loreclezole were evaluated during a long-term follow-up trial targeting higher plasma concentrations than those of the preceding controlled trial, and the result is better than in the double-blind trial.
14 citations
TL;DR: It is suggested that loreclezole represents a new class of agents which modulate GABAergic transmission via a unique interaction with the GABA receptor complex.
Abstract: The interaction of loreclezole (a structurally novel non-benzodiazepine anticonvulsant), diazepam, phenobarbital sodium, and ethosuximide with the benzodiazepine antagonists β-CCE, Ro 15-1788, and CGS 8216 and the purine antagonist aminophylline were examined in the rat i.v. metrazol seizure test. The anticonvulsant activity of loreclezole was inhibited by β-CCE and CGS 8216 but not by Ro 15-1788 or aminophylline. The inhibition produced by CGS 8216 was dose dependent (ID50 = 0.04 mg/kg i.p. CGS 8216) and surmountable. When the interactions of the various antagonists with loreclezole were compared to those of diazepam, phenobarbital sodium, and ethosuximide, a clear differentiation of activity was evident. β-CCE blocked the anticonvulsant activity of all four compounds whereas Ro 15-1788 blocked only the anticonvulsant effects of diazepam. CGS 8216 blocked the anticonvulsant effects of diazepam and loreclezole in a similar manner while being much less effective against the anticonvulsant effects of ethosuximide and ineffective against phenobarbital sodium. Aminophylline blocked the anticonvulsant effects of only ethosuximide. Based on these data and the anticonvulsant profile of loreclezole, we suggest that loreclezole represents a new class of agents which modulate GABAergic transmission via a unique interaction with the GABA receptor complex.
11 citations
TL;DR: The seizure frequency in the total group of drug-resistant epilepsy patients received loreclezole decreased and a reduction of 50% or more was observed in four patients.
8 citations