Experimental oral anticoagulation by a directly acting thrombin inhibitor (RGH-2958).
D-Phenylalanyl-L-prolyl-L-arginine aldehyde sulfate (RGH-2958), a directly acting synthetic thrombin inhibitor proved to be effective by experimental oral application. The rapid onset of its action has a special importance both from theoretical and practical point of view. Its antiplatelet effect relates to thrombin induced PA and runs parallel with the anticoagulant effect. RGH-2958 significantly reduced the thrombus weight in an experimental thrombosis model in rabbits. In the light of the therapeutic indices of the compound there is a real possibility to open a third way in the prevention and therapy of thrombosis.
Bagdy
D
D
Institute for Drug Research, Budapest, Hungary.
Barabás
E
E
Fittler
Z
Z
Orbán
E
E
Rabloczky
G
G
Bajusz
S
S
Széll
E
E
D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism; D001780:Blood Coagulation Tests; D004285:Dogs; D004355:Drug Stability; D004386:Duodenum / Q000378:metabolism; D005750:Gastric Juice / Q000378:metabolism; D007408:Intestinal Absorption; D009842:Oligopeptides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011817:Rabbits; D013917:Thrombin / Q000037:antagonists & inhibitors*; D013927:Thrombosis / Q000097:blood
D009842:Oligopeptides; C035202:H-D-Phe-Pro-arginal; D013917:Thrombin