BYK 191023 (hydrochloride)

选择性iNOS抑制剂（人重组iNOS、nNOS和eNOS的IC50s分别为0.086、17和162μM）；抑制iNOS诱导的RMC、RAW和HEK293细胞中亚硝酸盐的生成（IC50s分别为33、3.1和13μM）；抑制LPS诱导的大鼠血浆硝酸盐和亚硝酸盐水平升高（ED50=14.9μmol/kg每小时）；预防50μmol/kg每小时LPS诱导的内毒血症大鼠模型出现延迟性低血压；增加绵羊脓毒症休克模型中的平均动脉压和肾血流量。A selective iNOS inhibitor (IC50s = 0.086, 17, and 162 μM for human recombinant iNOS, nNOS, and eNOS, respectively); inhibits iNOS-induced nitrite generation in RMC, RAW, and HEK293 cells (IC50s = 33, 3.1, and 13 μM, respectively); suppresses LPS-induced increases in plasma nitrate and nitrite levels in rats (ED50 = 14.9 μmol/kg per hour); prevents development of delayed hypotension in a rat model of LPS-induced endotoxemia at 50 μmol/kg per hour; increases mean arterial pressure and renal blood flow in a sheep model of septic shock.