Peptides and/or proteins and their use in the preparation of a therapeutical and/or prophylactic pharmaceutical formulation

摘要

Peptides or proteins (I), based on the alpha - and beta -chain sequences of fibrin/fibrinogen, or their salts, amides and/or mixtures with each other or other materials, have therapeutic and/or preventive use in human or veterinary medicine. Peptides or proteins of formula R 1R 2N-CH 2-C(O)-Z 1-Z 2 (I), or their salts, amides and/or mixtures with each other or other materials, have therapeutic and/or preventive use in human or veterinary medicine. R 1, R 2H or up to 10C saturated or unsaturated hydrocarbyl; Z 1histidine or proline residue; and Z 2arginine residue or a peptide or protein residue (preferably of 2-30 aminoacids) having an initial arginine residue. An independent claim is included for medicaments containing (I). ACTIVITY : Antiinflammatory; antibacterial; immunosuppressive; Antirheumatic; Antiarteriosclerotic; vasotropic; Thrombolytic; anticoagulant; cytostatic; antipsoriatic. In tests for inhibition of reperfusion damage after surgically induced ischemia in rat cardiac tissue, intravenous administration of Gly-His-Arg-Pro-Leu-Asp-Lys-Lys-Arg-Glu-Glu-Ala-Pro-Ser-Leu-Arg-Pro-Ala-Pro-Pro-Pro-Ile-Ser-Gly-Gly-Gly-Tyr-Arg (Ia) at 800 Microg/kg reduced the precentage of dead tissue from 46% to 29%. MECHANISM OF ACTION : Fibrin antagonist; inhibition of fibrin-mediated adhesion of cells from the blood-stream onto vascular endothelium and/or migration of such cells into tissue; inhibition of deposition and adhesion of fibrin cleavage fragments on vascular walls.