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Titolo:
THE ABILITY OF THROMBIN INHIBITORS TO REDUCE THE THROMBIN ACTIVITY GENERATED IN PLASMA ON EXTRINSIC AND INTRINSIC ACTIVATION
Autore:
PRASA D; SVENDSEN L; STURZEBECHER J;
Indirizzi:
UNIV JENA KLINIKUM,ZENTRUM VASK BIOL & MED,NORDHAUSER STR 78 D-99089 ERFURT GERMANY PENTAPHARM LTD CH-4002 BASEL SWITZERLAND
Titolo Testata:
Thrombosis and haemostasis
fascicolo: 3, volume: 77, anno: 1997,
pagine: 498 - 503
SICI:
0340-6245(1997)77:3<498:TAOTIT>2.0.ZU;2-J
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHLOROMETHYL KETONE; ANTICOAGULANT ACTIVITY; RECOMBINANT HIRUDIN; PEPTIDE INHIBITORS; BINDING DOMAIN; FACTOR-XA; HEPARIN; ANTITHROMBIN; INTERRUPTION; BLOOD;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
53
Recensione:
Indirizzi per estratti:
Citazione:
D. Prasa et al., "THE ABILITY OF THROMBIN INHIBITORS TO REDUCE THE THROMBIN ACTIVITY GENERATED IN PLASMA ON EXTRINSIC AND INTRINSIC ACTIVATION", Thrombosis and haemostasis, 77(3), 1997, pp. 498-503

Abstract

In a thrombin generation test with continuous registration of thrombin activity in plasma we studied the ability of a variety of thrombin inhibitors of different type and mechanism of action to influence the activity of thrombin after activation of the coagulation system. Depending on the inhibitor, the peak of thrombin activity is delayed and/or reduced. By blocking the active site of generated thrombin inhibitors cause a concentration dependent reduction of the thrombin peak and inhibit feed-back reactions of thrombin resulting in a delay of thrombin generation. Highly potent synthetic active-site directed inhibitors (K-i less than or equal to 20 nM) reduce the thrombin activity formed inplasma after extrinsic or intrinsic activation with the same efficiency (IC50 0.1 - 0.6 mu M) as hirudin. The delay and reduction of thrombin generation by inhibitors of the anion-binding exosite 1 of thrombinis only attributed to an inhibition of feed-back reactions of thrombin. For a 50% reduction of thrombin activity in plasma by this type of inhibitors relatively high concentrations were determined.

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Documento generato il 20/09/20 alle ore 04:48:37