Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5814779 | Neuropharmacology | 2013 | 9 Pages |
Abstract
⺠Two pyridazine- and pyridine-derived GSMs were profiled in vitro and in rats. ⺠These GSMs are orally bioavailable and brain penetrant. ⺠These GSMs achieved >100-fold selectivities against Notch. ⺠These GSMs demonstrated Aβ42-lowering pIC50s as 7.0 and 7.2 in vitro. ⺠Thirty mg/kg single dose PO, maintained >20% brain Aβ42 reduction over 24 h in rats.
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Authors
Yunhong Huang, Ting Li, Andrew Eatherton, William L. Mitchell, Na Rong, Liang Ye, Xiu-Juan Yang, Shiyi Jin, Yu Ding, Jinqiang Zhang, Yi Li, Yiwen Wu, Yun Jin, Yingxia Sang, Ziqiang Cheng, Edward R. Browne, David C. Harrison, Ishrut Hussain,