A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABA
A
receptors which are partial or full inverse agonists of an &agr;5 receptor subunit while being relatively free of activity at &agr;1 and/or &agr;2 and/or &agr;3 receptor subunit binding sites; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of procon-vulsant activity.
一类取代
咪唑啉[5,1-a]
萘嗪衍
生物,作为
GABAA受体的
配体,它们是α5受体亚单位的部分或完全反向激动剂,同时在α1和/或α2和/或α3受体亚单位结合位点上相对缺乏活性;因此,它们对于增强认知有益,但可以减少或消除抗抗痉挛活性。