2,3-苯并二氮杂䓬（CFM）非竞争性AMPA受体拮抗剂的设计与开发
Design and development of 2,3-benzodiazepine (CFM) noncompetitive AMPA receptor antagonists.
作者信息
Gitto Rosaria, Zappal Maria, De Sarro Giovambattista, Chimirri Alba
机构信息
Dipartimento Farmaco-Chimico, Università di Messina, Italy.
出版信息
Farmaco. 2002 Feb;57(2):129-34. doi: 10.1016/s0014-827x(01)01186-7.
2,3-Benzodiazepines represent a class of heterocyclic compounds that interact with AMPA-type glutamate receptors in a noncompetitive manner. These compounds have attracted great interest for their pharmacological effects against acute and chronic neurodegenerative diseases, such as ischemia and epilepsy. We synthesized a large number of 2,3-benzodiazepine derivatives, which showed anticonvulsant properties in different seizure models and a noncompetitive blockade of AMPA receptor. This article will briefly mention our work in this field and the main SAR considerations.
2,3-苯并二氮杂䓬是一类以非竞争性方式与AMPA型谷氨酸受体相互作用的杂环化合物。这些化合物因其对急性和慢性神经退行性疾病（如缺血和癫痫）的药理作用而备受关注。我们合成了大量的2,3-苯并二氮杂䓬衍生物，它们在不同的癫痫模型中表现出抗惊厥特性以及对AMPA受体的非竞争性阻断作用。本文将简要介绍我们在该领域的工作以及主要的构效关系考量因素。
Zotero 插件