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- W4210733894 abstract "A series of novel procaine derivatives for intravenous anesthesia were prepared and evaluated by physicochemical properties and pharmacodynamic experiments in vivo and in vitro. Systematic optimization of procaine led to the identification of 6f, 6g, 6h, 6o, 6p and 6q with higher TI value and moderate log D. Compared with procaine (TI = 1.65), most procaine derivatives demonstrated better security, among whichcompound 6h (TI = 2.68)was the most notable one and showed fewer adverse events in animals. The result of hNR2B-HEK293 assay indicated that compound 6h suppressed the NMDA receptor 2B subtype channel activity and it showed more than 80% inhibitory effect at the concentration of 500 μM." @default.
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- W4210733894 date "2022-03-01" @default.
- W4210733894 modified "2023-10-18" @default.
- W4210733894 title "Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia" @default.
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- W4210733894 doi "https://doi.org/10.1016/j.bmcl.2022.128587" @default.
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