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Thromb Haemost 1979; 42(03): 1039-1045
DOI: 10.1055/s-0038-1656995
Original Article
Schattauer GmbH Stuttgart

Kinetic Studies on the Selectivity of a Synthetic Thrombin-Inhibitor Using Synthetic Peptide Substrates

A Huikata
*   The Departement of Physiology, Kobe University School of Medicine, Kobe, Japan
,
S Okamoto
*   The Departement of Physiology, Kobe University School of Medicine, Kobe, Japan
,
R Kikumoto
**   The Central Research Laboratory, Mitsubishi Chemical Industries, Ltd., Tokyo, Japan
,
Y Tamao
**   The Central Research Laboratory, Mitsubishi Chemical Industries, Ltd., Tokyo, Japan
› Institutsangaben
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Publikationsverlauf

Received 17. Dezember 1978

Accepted 13. März 1979

Publikationsdatum:
23. August 2018 (online)

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Summary

The synthetic thrombin-inhibitor termed No. 205 (N-α-dansyl-L-arginine-4-ethyl-piperidine amide) found in our laboratories was studied kinetically using synthetic peptide substrates. The following results were obtained. 1. No. 205 inhibited thrombin competitively with bz-Phe-Val-Arg-pNA and the Ki value obtained was extremely small, 3.7 × 10-8 M. 2. No. 205 also inhibited trypsin competitively with bz-Phe-Val-Arg-pNA but the Ki value obtained was far larger than that for thrombin, 1.0 × 10-5 M. 3. No. 205 inhibited F. Xa, plasmin and urokinase only to a small extent when estimated using 2 × 10-4 M D-Val-Leu- Lys-pNA, bz-Ile-Glu-Gly-Arg-pNA and Glu-Gly-Arg-pNA, respectively. 4. No. 205 differed from APPA in its specific inhibitory spectrum for thrombin as compared to trypsin, plasmin and F. Xa. The above results indicate that No. 205 is an extremely potent and highly selective reversible thrombin-inhibitor.

 

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