Lefer A M, Messenger M
Arzneimittelforschung. 1982;32(9):1089-91.
3-Methyl-(1-[2-naphthyloxy]-ethyl)-2-pyrazolin-5-one (nafazatrom), a new antithrombotic agent, at doses of 0.5 to 2.0 mg/kg significantly prolonged survival of rats after induction of traumatic shock. Nafazatrom did not exert significant effects on arterial blood pressure in either control or shock animals. However, nafazatrom significantly prevented the plasma accumulation of the lysosomal protease cathepsin D and of the cardiotoxic peptide, myocardial depressant factor (MDF). In addition, nafazatrom (10 microgram/ml) significantly stabilized lysosomal membranes in isolated liver lysosomal suspensions, and inhibited proteolysis in pancreatic homogenates. Thus, nafazatrom exerts significant anti-shock activity which appears to be related to its favorable cellular and metabolic effects.
3-甲基-(1-[2-萘氧基]-乙基)-2-吡唑啉-5-酮(萘呋胺酯)是一种新型抗血栓形成剂,以0.5至2.0毫克/千克的剂量可显著延长创伤性休克诱导后大鼠的存活时间。萘呋胺酯对对照组或休克动物的动脉血压均无显著影响。然而,萘呋胺酯可显著抑制溶酶体蛋白酶组织蛋白酶D和心脏毒性肽心肌抑制因子(MDF)在血浆中的蓄积。此外,萘呋胺酯(10微克/毫升)可显著稳定离体肝脏溶酶体悬浮液中的溶酶体膜,并抑制胰腺匀浆中的蛋白水解作用。因此,萘呋胺酯具有显著的抗休克活性, 这似乎与其良好的细胞和代谢作用有关。