Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Most Clot-Bound Thrombin Activity is Inhibited by Plasma Antithrombin during Clot Aging, but a Very Small Fraction Survives
Yasuhiko KOMATSUHideya HAYASHI
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2000 年 23 巻 4 号 p. 502-505

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Inhibitory effects of thrombin inhibitors against clot-bound throumbin have been evaluated using clots prepared from human plasma as the source of clot-immobilized active enzyme, and the clot-bound thrombin has been reported to be protected from its inhibition by antithrombin. However, we found that the clot-bound thrombin was not intrinsically protected from inhibition by antithrombin, i.e., a large fraction of intially active clotbound thrombin mas inhibited by antithrombin present in human plasma time dependently, and only very small fractions (0.04-0.08%) of the thronbin retained their enzymatic activity after clot-aging. These results suggest that the extent of clot-aging determines the sensitivity of clot-bound thrombin to antithrombin, and that inhibitory effects of drugs against clot-bound thrombin in vitro must be interpreted with caution to estimate their effects in vivo.
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© The Pharmaceutical Society of Japan
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