Binding of low molecular weight heparin (Tinzaparin sodium) to bovine endothelial cells in vitro
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Binding of low molecular weight heparin (Tinzaparin sodium) to bovine endothelial cells in vitro. / Larnkjær, Anni; Østergaard, Per B.; Flodgaard, Hans J.
In: Thrombosis Research, Vol. 75, No. 2, 1994, p. 185-194.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Binding of low molecular weight heparin (Tinzaparin sodium) to bovine endothelial cells in vitro
AU - Larnkjær, Anni
AU - Østergaard, Per B.
AU - Flodgaard, Hans J.
N1 - (Ekstern)
PY - 1994
Y1 - 1994
N2 - Heparinase depolymerized low molecular weight (LMW) heparin (Tinzaparin sodium, Logiparin®) was radiolabelled by catalytic tritiation to high specific radioactivity and the binding to fetal bovine heart endothelial (FBHE) cells was studied at 4°C and 37°C. The binding was found to be time dependent and saturable. Two classes of binding sites could be distinguished from Scatchard analysis at both temperatures: One with high affinity (KD = 0.027 μM at 4°C, KD = 0.012 μM at 37°C) and another with very low affinity (KD = 69 μM at 4°C and 37 μM at 37°C). The binding reversibility was affected by the temperature indicating internalization of a fraction of the bound LMW heparin. At 4°C only 11% of the specifically bound heparin was bound irreversibly. At 37°C the non displaceable fraction accounted for 28 % of the specifically bound LMW heparin. This work demonstrates that tinzaparin sodium binds specifically to endothelial cells. This binding may be useful in interpreting pharmacokinetic properties of this low molecular weight heparin.
AB - Heparinase depolymerized low molecular weight (LMW) heparin (Tinzaparin sodium, Logiparin®) was radiolabelled by catalytic tritiation to high specific radioactivity and the binding to fetal bovine heart endothelial (FBHE) cells was studied at 4°C and 37°C. The binding was found to be time dependent and saturable. Two classes of binding sites could be distinguished from Scatchard analysis at both temperatures: One with high affinity (KD = 0.027 μM at 4°C, KD = 0.012 μM at 37°C) and another with very low affinity (KD = 69 μM at 4°C and 37 μM at 37°C). The binding reversibility was affected by the temperature indicating internalization of a fraction of the bound LMW heparin. At 4°C only 11% of the specifically bound heparin was bound irreversibly. At 37°C the non displaceable fraction accounted for 28 % of the specifically bound LMW heparin. This work demonstrates that tinzaparin sodium binds specifically to endothelial cells. This binding may be useful in interpreting pharmacokinetic properties of this low molecular weight heparin.
KW - Binding study
KW - Endothelial cells
KW - LMW heparin
UR - http://www.scopus.com/inward/record.url?scp=0028061213&partnerID=8YFLogxK
U2 - 10.1016/0049-3848(94)90067-1
DO - 10.1016/0049-3848(94)90067-1
M3 - Journal article
C2 - 7974392
AN - SCOPUS:0028061213
VL - 75
SP - 185
EP - 194
JO - Thrombosis Research
JF - Thrombosis Research
SN - 0049-3848
IS - 2
ER -
ID: 249247449