ONO - 5046，一种新型人中性粒细胞弹性蛋白酶抑制剂。
ONO-5046, a novel inhibitor of human neutrophil elastase.
作者信息
Kawabata K, Suzuki M, Sugitani M, Imaki K, Toda M, Miyamoto T
机构信息
Minase Research Institute, Ono Pharmaceutical Co., Ltd., Osaka, Japan.
出版信息
Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20. doi: 10.1016/0006-291x(91)91862-7.
ONO-5046, N-[2-[4-(2,2-Dimethylpropionyloxy)phenylsulfonylamino] aminoacetic acid, competitively inhibited human neutrophil elastase (IC50 = 0.044 microM, Ki = 0.2 microM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. However, ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase.
ONO - 5046，N - [2 - [4 - (2,2 - 二甲基丙酰氧基)苯基磺酰氨基]氨基乙酸，可竞争性抑制人中性粒细胞弹性蛋白酶（IC50 = 0.044微摩尔，Ki = 0.2微摩尔）。它还能抑制从兔、大鼠、仓鼠和小鼠中获得的白细胞弹性蛋白酶。然而，即使在100微摩尔浓度下，ONO - 5046也不抑制胰蛋白酶、凝血酶、纤溶酶、血浆激肽释放酶、胰腺激肽释放酶、糜蛋白酶和组织蛋白酶G。在体内研究中，通过气管内给药，ONO - 5046可抑制仓鼠的肺出血（ID50 = 82微克/千克）；通过静脉给药，可抑制豚鼠皮肤毛细血管通透性增加（ID50 = 9.6毫克/千克），这两种情况均由人中性粒细胞弹性蛋白酶诱导产生。
Zotero 插件