| Autor: |
Kemme, Michiel J.B., Schoemaker, Rik C., Burggraaf, Jacobus, van der Linden, Monique, Noordzij, Marina, Moerland, Matthijs, Kluft, Cornelis, Cohen, Adam F. |
| Předmět: |
|
| Zdroj: |
Journal of Pharmacokinetics & Pharmacodynamics; Feb2003, Vol. 30 Issue 1, p3, 20p, 2 Diagrams, 12 Graphs |
| Abstrakt: |
Binding of tissue plasminogen activator (t-PA) to the endothelium may be important in the prevention of thrombus formation. The aim was to develop a method to quantify endothelial binding in vivo. Nine healthy male volunteers received a 40 min continuous infusion with low dose recombinant t-PA (3.75 µg/min) and an indocyanine green infusion (0.5 mg/min) as control. A three-compartment recirculatory model was developed to account for non-specific circulatory delay effects, t-PA antigen, activity and t-PA/PAI-1 complex profiles showed a marked delay in increase at the beginning of the infusion. A reversible and concentration-dependent binding component was incorporated in the model which resulted in an accurate description of the t-PA concentration profile. t-PA binding was characterized by a dissociation constant of 5.9 ng/ml (SEM 1.8, CV 0%; fixed) and a binding capacity of 70 µg t-PA (SEM 10, CV 48%). This model can be used as a tool to quantify the ability of the endothelium to bind t-PA. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
|
Full text from SpringerLink