Thromb Haemost 1972; 28(03): 351-358
DOI: 10.1055/s-0038-1649018
Original Article
Schattauer GmbH

The Effects of Some Synthetic Compounds on In Vitro Fibrinolytic Activity Measured by Different Methods and the Relevance to Activity In Vivo

A.J Baillie**
1   From Inveresk Research International, Musselburgh, Scotland
,
A. K Sim
1   From Inveresk Research International, Musselburgh, Scotland
› Author Affiliations
Further Information

Publication History

Publication Date:
24 July 2018 (online)

Summary

The activity of several synthetic compounds, rated from good to poor (or inactive) fibrinolytic activators, has been assessed by two different commonly-used in vitro methods. Compounds shown to be active over a narrow concentration range in the hanging clot test were shown to be inhibitors of plasmin and trypsin in the casein-olytic test. The inhibitory activity of these compounds was shown to increase with increasing substrate concentration and apparent activity in the hanging clot test. Possible explanations and relevance of these observations are discussed.

** Present address: Department of Pharmaceutical Technology, University of Strathclyde, Glasgow, Scotland.


 
  • References

  • 1 Baillie A. J, and Sim A. K. 1971; Activation of the fibrinolytic enzyme system in laboratory animals and in man. A comparative study. Thrombosis et Diathesis Haemorrhagica 25: 499.
  • 2 Brown J. H, and Pollock S. H. 1970; Activation of trypsin by anti-inflammatory drugs. Proceedings of the Society for Experimental Biology and Medicine 135: 796.
  • 3 Chignell C. F. 1969; Interaction of flufenamic acid and other N-aryl-anthranilates with serum albumin. Molecular Pharmacology 5: 455.
  • 4 Gryglewski R. J. 1966; The fibrinolytic activity of anti-inflammatory drugs. Journal of Pharmacy and Pharmacology 18: 474.
  • 5 Geyglewski R. J. 1970. On the mechanism of fibrinolysis induced by anti-inflammatory drugs. In: Schor J. M. (Ed.) Chemical Control of Fibrinolysis. Wiley-Interscience; New York,: 43.
  • 6 Isacson S, and Nilsson I. M. 1970; Effect of treatment with combined phenformin and ethyloestrenol on the coagulation and fibrinolytic systems. Scandinavian Journal of Haematology 7: 404.
  • 7 von Kaulla K. N. 1965; Simple test tube arrangements for screening fibrinolytic activity of synthetic organic compounds. Journal of Medicinal Chemistry 8: 164.
  • 8 von Kaulla K. N, and Ens G. 1967; On the structure related properties of synthetic organic clot-dissolving compounds. Biochemical Pharmacology 16: 1023.
  • 9 von Kaulla K. N. 1968; Structure dependent fibrinolytic activity of anti-inflammatory drugs and related compounds. Arzneimittel-Forschung 18: 409.
  • 10 von Kaulla K. N. 1970. On the in vitro mechanism of synthetic fibrinolytic agents. In: Schor J. M. (Ed.) Chemical Control of Fibrinolysis. Wiley-Interscience; New York: 1.
  • 11 McNicol G. P, and Douglas A. S. 1964. The fibrinolytic enzyme system. In: Dyke S. C. (Ed.) Recent Advances in Clinical Pathology. Series 4 Churchill; London:
  • 12 Ungar G, and Ungar A. L. 1966; Protease changes in transplanted skin. Proceedings of the Society for Experimental Biology and Medicine 121: 1098.
  • 13 Whitehouse M. W. 1968 The molecular pharmacology of anti-inflammatory drugs, some possible mechanisms of action at the biochemical level. Biochemical Pharmacology Supplement. 293