• Publications
  • Influence
Activity of 2,3-benzodiazepines at Native Rat and Recombinant Human Glutamate Receptors In Vitro: Stereospecificity and Selectivity Profiles
Results indicate that 2,3-benzodiazepines are potent, selective and stereospecific antagonists of the AMPA subtype of the non-NMDA glutamate receptor. Expand
Blockers of voltage-gated sodium channels for the treatment of central nervous system diseases.
This review focuses on the current trends in sodium channel research, surveying the traditional and newly emerging therapeutic fields, and the diverse medicinal chemistry of sodium channel blockers. Expand
Structure-activity relationships of 2,3-benzodiazepine compounds with glutamate antagonistic action
Abstract A series of N-substituted 1-(4'-aminophenyl)-4-methyl-3,4-dihydro-7,8-methylene-dioxy5H-2,3-benzodiazepines, structural analogues of the selective non-NMDA antagonist GYKI 52466, has beenExpand
Tolperisone-Type Drugs Inhibit Spinal Reflexes via Blockade of Voltage-Gated Sodium and Calcium Channels
The data suggest that tolperisone-type muscle relaxants exert their spinal reflex inhibitory action predominantly via a presynaptic inhibition of the transmitter release from the primary afferent endings via a combined action on voltage-gated sodium and calcium channels. Expand
Comparison of spontaneous and evoked epileptiform activity in three in vitro epilepsy models
The contribution of NMDA and AMPA types of glutamate receptors to the development and maintenance of epileptiform activity in cortical cell assemblies is different in the three models, and changes in the membrane characteristics of neurones play a crucial role in the increased excitability. Expand
NR2B containing NMDA receptor dependent windup of single spinal neurons
Results are in agreement with the well-documented effectivity of NR2B subtype selective NMDA receptor antagonists in chronic pain models and give the first direct evidence that spinal mechanisms are involved in this effect. Expand
Structural analogues of some highly active non-competitive AMPA antagonists.
Some 5-methyl analogues of the non-competitive AMPA antagonists 3-acylated 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3H-2,3-benzodi azepines have been synthesized and reveal effects comparable to those of GYKI 52466. Expand
Non-competitive AMPA antagonists of 2,3-benzodiazepine type.
This review summarises the present knowledge about the allosteric site, dubbed "GYKI site" where the 2,3-benzodiazepines are supposed to bind to and the main fields of their clinical utility are outlined with special regard to talampanel in the light of the ongoing clinical trials with this new drug candidate. Expand
New non competitive AMPA antagonists.
It was found that chloro-, dichloro- and bromo-substitutions in the benzene ring and additionally imidazole ring condensation on the diazepine ring can successfully substitute the methylenedioxy group in the well known molecules GYKI 52466 and GYki 53773 and the 3-acetyl-4-methyl structural feature in 2, respectively, preserving the highly active AMPA antagonist characteristic of the original molecules. Expand