激肽释放酶
仓鼠
弹性蛋白酶
组织蛋白酶G
中性粒细胞弹性蛋白酶
化学
纤溶酶
体内
药理学
生物化学
胰蛋白酶
分子生物学
生物
酶
炎症
免疫学
生物技术
作者
Kazuhito Kawabata,Mayumi Suzuki,Masafumi Sugitani,Katsuhiro Imaki,Masaaki Toda,Tsumoru Miyamoto
标识
DOI:10.1016/0006-291x(91)91862-7
摘要
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.
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