Table 3. Effect of dabigatran, argatroban, DAPA or hirudin on 125I-thrombin binding to fibrin clots.
Binding of 125I-thrombin to γA/γA- or γA/γ′-fibrin clots in the absence or presence of dabigatran, argatroban, DAPA, or hirudin was determined by measuring the amount of 125I-thrombin in the supernatants of compacted clots prepared by incubating γA/γA- or γA/γ′-fibrinogen with a catalytic amount of batroxobin. EC50 values were determined by nonlinear regression analysis and converted to Ki values by correction for Kd of 125I-thrombin for fibrin. Change denotes the maximal change in the percentage of bound 125I-thrombin compared with that in the absence of inhibitor.
| Dabigatran | Argatroban | DAPA | Hirudin | |||||
|---|---|---|---|---|---|---|---|---|
| Ligand | Ki (nM) | Change (%) | Ki (nM) | Change (%) | Ki (nM) | Change (%) | Ki (nM) | Change (%) |
| γA/γA-fibrin | 3.8 ± 1.5 | -21.4 ± 3.3 | 2.4 ± 1.9 | +18.3 ± 5.0 | 2.1 ± 0.9 | +17.0 ± 2.7 | 3.4 ± 0.3 | -100 |
| γA/γ′-fibrin | 26.0 ± 4.0 | -9.4 ± 1.4 | 7.0 ± 5.6 | +26.1 ± 0.4 | 19.6 ± 19.1 | +20.1 ± 3.6 | 3.4 ± 0.1 | -100 |