Abstract:A series of imidazodiazepines has been developed that possess reduced sedative liabilities but retain efficacy in anticonvulsant screening models. The latest of these compounds, (5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazole [1,5-α][1,4]diazepin-3-yl) oxazole known as KRM-II-81) is currently awaiting advancement into the clinic. A deuterated structural analog (D5-KRM-II-81) was
diazepin-3yl)oxazole GABAAR -GABA A receptor hERG -human Ether a-go-go related gene = KCNH2 KPP-III-34: 2-(8-bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5α][1,4]diazepin-3yl)-4-ethyloxazole This article has not been copyedited and formatted. The final version may differ from this version.
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