Effects of [(N-alkyl-1,3-dioxo-1H,3H-isoindolin-5-yl)oxy]alkanoic acids, [(N-alkyl-1-oxo-1H,3H-isoindolin-5-yl)oxy]butanoic acids, and related derivatives on chloride influx in primary astroglial cultures
作者:Steven D. Wyrick、Forrest T. Smith、W. Evans Kemp、Anne A. Grippo
DOI:10.1021/jm00393a020
日期:1987.10
agents that inhibit chloride influx and therefore lower intracellular chloride levels in a major cell type in cerebral gray matter, the astrocyte, inhibit astrocytic swelling in vitro and in vivo. In our laboratories, 4-[(N-alkyl-1,3-dioxo-1H,3H-isoindolin-5-yl)oxy]alkanoic acids and related derivatives have been synthesized and tested for ability to lower intracellular astrocytic chloride levels in an established
业已表明,抑制氯离子流入并因此降低脑灰质星形细胞中主要细胞类型的细胞内氯水平的试剂在体外和体内均抑制星形胶质细胞的肿胀。在我们的实验室中,已经合成了4-[((N-烷基-1,3-二氧杂-1H,3H-异吲哚基-5-基)氧基]链烷酸和相关衍生物,并测试了降低细胞内星形细胞氯化物水平的能力。建立了体外培养的大鼠星形胶质细胞模型。通常,具有氮取代基(例如相对小的烷基)的衍生物在0.1 mM和/或0.5 mM的水平上具有活性,而较大的取代基(例如环戊基和环己基)的活性较低。芳环上的卤素取代没有增强活性。