Efaproxiral

一种别构性血红蛋白修饰剂，能够降低血红蛋白对氧的亲和力，增加氧气从血液到组织的扩散；在1.75mM浓度下，在26mmHg的pO2条件下，将分离人全血中的p50从26.75mm Hg增加到38.63mm Hg，将血红蛋白-氧饱和度从48%降低至33.8%；在150mg/kg剂量下，在RIF-1小鼠纤维肉瘤侧腹肿瘤模型中，给药30分钟后将肿瘤pO2从5.2mm Hg提高至13.1mm Hg；在100 μM浓度下，增强EMT6小鼠乳腺癌细胞在缺氧条件下的辐射诱导细胞毒性；在100mg/kg剂量下，在缺氧Lewis肺肿瘤小鼠模型中增加辐射增敏性并抑制肿瘤生长；在150mg/kg剂量下，增加正常小鼠及LCA结扎引起心肌梗死小鼠的运动能力。An allosteric Hb modifier that reduces the affinity of Hb for oxygen, increasing the diffusion of oxygen from blood to tissue; increases p50 from 26.75 to 38.63 mm Hg and decreases the percent Hb-O2 saturation from 48 to 33.8% at a pO2 of 26 mm Hg in isolated human whole blood at 1.75 mM; increases tumor pO2 from 5.2 to 13.1 mm Hg 30 minutes after administration in a RIF-1 mouse fibrosarcoma flank tumor model at 150 mg/kg; enhances radiation-induced cytotoxicity in EMT6 mouse breast cancer cells grown under hypoxic conditions at 100 μM; increases radiosensitization and inhibits tumor growth in a hypoxic Lewis lung tumor mouse model at 100 mg/kg; increases the running capacity of normal mice and mice with LCA ligation-induced MI at 150 mg/kg.