Antithrombotic activity of a novel C-terminal hirudin analog in experimental animals.
A synthetic hirudin55-65 C-terminal fragment analog was evaluated for anticoagulant activity and in models of experimental thrombosis in mice and rats. Intravenous injection caused dose-related inhibition of thrombin and anticoagulation in rat blood samples, protection from thromboembolism in mice and inhibition of stasis-induced venous thrombosis in rats. Antithrombotic effectiveness corresponded with anticoagulant activity. Anephric animals exhibited longer duration of activity than normal animals suggesting the kidney as a major route of elimination.
Broersma
R J
RJ
Merrell Dow Research Institute, Indianapolis, IN.
Kutcher
L W
LW
Heminger
E F
EF
Krstenansky
J L
JL
Marshall
F N
FN
D000595:Amino Acid Sequence; D000818:Animals; D000925:Anticoagulants; D001777:Blood Coagulation / Q000187:drug effects; D005343:Fibrinolytic Agents; D008297:Male; D051379:Mice; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013923:Thromboembolism / Q000517:prevention & control; D013924:Thrombophlebitis / Q000188:drug therapy
D000925:Anticoagulants; D005343:Fibrinolytic Agents; D009842:Oligopeptides; C064762:MDL 28050