Horváth K
Gyógyszerkutató Intézet Kft, 1045 Budapest, Berlini u. 47-49.
Acta Pharm Hung. 2001;71(1):73-9.
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.
药物研究所（IDR）合成并研究的2,3-苯二氮䓬类化合物（2,3-BDZs）在中枢神经系统活性化合物中代表了一个独特的家族。尽管具有共同的化学骨架，但2,3-BDZs在药理学上有所不同。在临床上无镇静作用的抗焦虑母体化合物托非索泮的基础上，已发现了在中枢神经系统中具有选择性结合位点特定分布的进一步衍生物。此外，还描述了具有兴奋特性的多巴胺摄取抑制剂。最后但最重要的是，还发现了具有异常广泛抗惊厥谱的化合物。从后一系列中，第一种非竞争性AMPA拮抗剂GYKI-52,466如今作为研究谷氨酸神经传递和谷氨酸拮抗剂治疗潜力的黄金标准。本文总结了2,3-BDZ家族最突出成员的主要药理作用。
