Highlights of CNS research at IDR: 2,3-benzodiazepines

2,3-Benzodiazepines (2,3-BDZs) synthesized and investigated at IDR represent a unique family among CNS active compounds. Though sharing common chemical backbone, 2,3-BDZs are pharmacologically different. Over the clinically nonsedative anxiolytic parent compound tofisopam, further derivatives with specific distribution of selective binding sites in the CNS have been found. Furthermore, dopamine-uptake inhibitors with stimulant character were also described. Finally but most importantly compounds with unusually broad anticonvulsant spectrum were also discovered. From this series the first non-competitive AMPA antagonist, GYKI-52466 serves today as the golden standard for investigating glutamate neurotransmission and the therapeutical potential of glutamate antagonists. The present paper summarizes the main pharmacological actions of the 2,3-BDZ family.