Schack L, Dietl T
Hoppe Seylers Z Physiol Chem. 1982 Jan;363(1):107-12.
In all mammals investigated so far, an amount of 0.1 - 1 biological unit (KU) of hog pancreatic kallikrein per kg body weight injected intravenously caused a fast reduction in blood pressure with one exception, the rat. Even 1000 times higher doses of hog pancreatic kallikrein did not reduce the blood pressure in this animal. In spite of many experiments performed with rats using hog pancreatic kallikrein to influence various metabolic pathways, there has been no proof, to date, that this enzyme also causes kallikrein-specific effects via kinin liberation in rats. We found only a slow and weak reduction of rat blood pressure after injection of 100 KU hog pancreatic kallikrein per rat, when the endogenous kininases had been previously inactivated by the kininase II inhibitor captopril. However, a fast reduction in blood pressure, similar to the response observed after kinin injection, could be recorded if 90 microliter rat blood, previously incubated for a few minutes with a least 20 k.u. hog pancreatic kallikrein in the presence of captopril, was reinjected. Hence, kinin liberation from rat kininogens by hog pancreatic kallikrein does occur, but proceeds so slowly that the fast kinin degradation by kininases can prevent the typical blood pressure effect of kinin in vivo.
在迄今所研究的所有哺乳动物中,每千克体重静脉注射0.1 - 1生物单位(KU)的猪胰激肽释放酶都会使血压迅速降低,但大鼠除外。即使剂量比这高1000倍的猪胰激肽释放酶也不会降低该动物的血压。尽管用猪胰激肽释放酶对大鼠进行了许多实验以影响各种代谢途径,但迄今为止,尚无证据表明这种酶在大鼠体内也通过激肽释放而产生激肽释放酶特异性效应。当用激肽酶II抑制剂卡托普利预先使内源性激肽酶失活后,我们发现每只大鼠注射100 KU猪胰激肽释放酶后,大鼠血压仅有缓慢而微弱的降低。然而,如果将90微升预先在卡托普利存在的情况下与至少20 k.u.猪胰激肽释放酶孵育几分钟的大鼠血液重新注射,则可记录到与注射激肽后观察到的反应相似的血压快速降低。因此,猪胰激肽释放酶确实能从大鼠激肽原中释放激肽,但过程非常缓慢,以至于激肽酶对激肽的快速降解能够在体内阻止激肽产生典型的血压效应。