Degradation of a benzamidine-type synthetic inhibitor of coagulation enzymes in plasma of various species.
The synthetic coagulation enzyme inhibitor N alpha-tosylglycyl-3-amidinophenylalanine methyl ester is anticoagulantly active in vitro in concentrations corresponding rather to its thrombin inhibiting activity than to its anti-factor Xa activity. The anticoagulant effect is not diminished by incubation in human plasma in vitro. In guinea pig and rat plasma, however, the inhibitor is hydrolysed, at different rates, yielding the corresponding N alpha-tosylglycyl-3-amidinophenylalanine, a less potent inhibitor of thrombin and factor Xa.
Hauptmann
J
J
Department of Pharmacology and Toxicology, Medical Academy Erfurt, Germany.
D000818:Animals; D000991:Antithrombins / Q000494:pharmacology*; D001550:Benzamidines / Q000494:pharmacology*; D001780:Blood Coagulation Tests; D004151:Dipeptides / Q000494:pharmacology*; D065427:Factor Xa Inhibitors; D006168:Guinea Pigs; D006207:Half-Life; D006801:Humans; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D013045:Species Specificity
D000991:Antithrombins; D001550:Benzamidines; D004151:Dipeptides; D065427:Factor Xa Inhibitors; D010880:Piperidines; C068769:N(alpha)-tosylglycyl-3-amidinophenylalanine methyl ester; C068770:N(alpha)-tosyl-glycyl-3-amidinophenylalanine; C035199:N(alpha)-tosyl-(3-amidinophenyl)alanine piperidide