[Highlights of CNS research at IDR: 2,3-benzodiazepines].
2,3-benzodiazepines (2,3-BDZs) synthesized and investigated at the Institute for Drug Research (IDR) represent a unique family among CNS active compounds. Though sharing common chemical backbone, 2,3-BDZs are pharmacologically different. Over the clinically non-sedative 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 latter series the first non-competitive AMPA antagonist, GYKI-52,466 serves today as the golden standard for investigating the glutamate neurotransmission and the therapeutical potential of glutamate antagonists. The present paper summarizes the main pharmacological actions of the most prominent members of the 2,3-BDZ family.
Horváth
K
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Gyógyszerkutató Intézet Kft, 1045 Budapest, Berlini u. 47-49.
D000047:Academies and Institutes; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry; D001569:Benzodiazepines; D002491:Central Nervous System Agents / Q000138:chemical synthesis* / Q000737:chemistry; D018765:Dopamine Uptake Inhibitors / Q000138:chemical synthesis; D006814:Hungary; D012106:Research / Q000639:trends; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D002491:Central Nervous System Agents; D018765:Dopamine Uptake Inhibitors; D001569:Benzodiazepines
Központi idegrendszerre ható gyógyszerek kutatása a GYKI-ban: egy sikeres vegyületcsalád, a 2,3-benzodiazepinek.