Rehse K, Herpel M, Piechocki D
Institut für Pharmazie, Freie Universität Berlin, Germany.
Arch Pharm (Weinheim). 1996 Feb;329(2):83-6. doi: 10.1002/ardp.19963290205.
Five 1-oximino-1-nitro compounds (nitrolic acids) were prepared and tested for antithrombotic and blood pressure lowering activities. 1-Nitro-ethanone 1-oxime (1, ethylnitrolic acid) 2 h after oral administration to rats inhibited thrombus formation by a laser beam in mesenteric arterioles of rats by 69% and by 46% in venules (60 mg/kg). The blood pressure of SHR rats even at this high dose only was decreased by 10% suggesting that antithrombotic and blood pressure effects can be dissociated. The in vitro decomposition of 1 at 37 degrees C nearly exclusively gave N2O and acetic acid indicating that HNO primarily had been formed.
制备了五种1-氧代亚氨基-1-硝基化合物(硝肟酸),并对其抗血栓形成和降血压活性进行了测试。给大鼠口服1-硝基乙酮1-肟(1,乙基硝肟酸)2小时后,在大鼠肠系膜小动脉中,通过激光束抑制血栓形成的作用达69%,在小静脉中为46%(60mg/kg)。即使在如此高剂量下,SHR大鼠的血压仅下降了10%,这表明抗血栓形成和血压作用是可以分开的。1在37℃下的体外分解几乎只产生N2O和乙酸,这表明主要生成了HNO。