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Titolo:
INHIBITION OF THROMBIN GENERATION IN PLASMA BY INHIBITORS OF FACTOR XA
Autore:
PRASA D; SVENDSEN L; STURZEBECHER JJ;
Indirizzi:
UNIV JENA,KLINIKUM,ZENTRUM VASKULARE BIOL & MED,NORDHAUSER STR 78 D-99089 ERFURT GERMANY PENTAPHARM LTD CH-4002 BASEL SWITZERLAND
Titolo Testata:
Thrombosis and haemostasis
fascicolo: 4, volume: 78, anno: 1997,
pagine: 1215 - 1220
SICI:
0340-6245(1997)78:4<1215:IOTGIP>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
TICK ANTICOAGULANT PEPTIDE; COAGULATION FACTOR-XA; BOVINE FACTOR-XA; SELECTIVE INHIBITOR; RECOMBINANT HIRUDIN; SYNTHETIC THROMBIN; STANDARD HEPARIN; IN-VITRO; BLOOD; POTENT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
D. Prasa et al., "INHIBITION OF THROMBIN GENERATION IN PLASMA BY INHIBITORS OF FACTOR XA", Thrombosis and haemostasis, 78(4), 1997, pp. 1215-1220

Abstract

A series of inhibitors of factor Xa (FXa) were investigated using thethrombin generation assay to evaluate the potency and specificity needed to efficiently block thrombin generation in activated human plasma. By inhibiting FXa the generation of thrombin in plasma is delayed and decreased. Inhibitor concentrations which cause 50 percent inhibition of thrombin generation (IC50) correlate in principle with the K-i values for inhibition of free FXa. Recombinant tick anticoagulant peptide (r-TAP) is able to inhibit thrombin generation with considerably lowIC50 values of 49 nM and 37 nM for extrinsic and intrinsic activation, respectively. However, the potent synthetic, low molecular weight inhibitors of FXa (K-i values of about 20 nM) are less effective in inhibiting the generation of thrombin with IC50 values at micromolar concentrations. The overall effect of inhibitors of FXa in the thrombin generation assay was compared to that of thrombin inhibitors. On the basis of similar K-i values for the inhibition of the respective enzyme, synthetic FXa inhibitors are less effective than thrombin inhibitors. In contrast, the highly potent FXa inhibitor r-TAP causes a stronger reduction of the thrombin activity in plasma than the most potent thrombin inhibitor hirudin.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/10/20 alle ore 12:06:56