Pâques E P, Römisch J
Research Laboratories of Behringwerke AG, Marburg, FRG.
Thromb Res. 1991 Oct 1;64(1):11-21. doi: 10.1016/0049-3848(91)90201-7.
The synthetic low molecular weight inhibitors MD 805, FUT-175 and FOY as well as heparin and r-Hirudin were compared for their in vitro antithrombotic potencies and protease specificities. The amidolytic activity of thrombin and the plasma coagulation were effectively inhibited by MD 805 and, in particular, by r-Hirudin. FUT-175 and FOY revealed only weak inhibition. None of the synthetic substances discriminated between alpha-, beta- and gamma-thrombin. Beside r-Hirudin only MD 805 revealed a relatively good specificity for thrombin. On the contrary, FUT-175 and FOY are unspecific and can not be classified as thrombin inhibitors.
比较了合成的低分子量抑制剂MD 805、FUT - 175和FOY以及肝素和重组水蛭素的体外抗血栓形成能力和蛋白酶特异性。MD 805,尤其是重组水蛭素可有效抑制凝血酶的酰胺水解活性和血浆凝固。FUT - 175和FOY仅表现出微弱的抑制作用。这些合成物质均不能区分α-、β-和γ-凝血酶。除重组水蛭素外,只有MD 805对凝血酶表现出相对较好的特异性。相反,FUT - 175和FOY是非特异性的,不能归类为凝血酶抑制剂。