[The pharmacodynamics of synthetic thrombin inhibitors of the basic type substituted n-alpha arylsulfonylated phenylalanine amide].
Nonspecific pharmacodynamic effects of synthetic thrombin inhibitors, basically substituted N alpha-arylsulfonylated phenylalanine amides, were studied in animal experiments. Upon intravenous bolus injection they exert a rapid fall in blood pressure, which limitates the tolerance. In contrast to the antithrombin activity, toxicity and side effects of the amidino compounds are not dependent on the position of the amidino group within the molecule. On the other hand, compounds with other basic groups, i.e. the amino, aminomethyl, and guanidinomethyl analogues are less toxic and less hypotensively active. The nonspecific pharmacodynamic effects of synthetic thrombin inhibitors of the benzamidine type must be caused by the highly basic amidino group (the benzamidine moiety) of the compounds.
D000578:Amidines / Q000494:pharmacology*; D000818:Animals; D001550:Benzamidines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001794:Blood Pressure / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D006339:Heart Rate / Q000187:drug effects; D007928:Lethal Dose 50; D051379:Mice; D010649:Phenylalanine / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D013917:Thrombin / Q000037:antagonists & inhibitors*
D000578:Amidines; D001550:Benzamidines; D010649:Phenylalanine; D013917:Thrombin
Untersuchungen zur Pharmakodynamik synthetischer Thrombininhibitoren vom Typ basisch substituierter N alpha-arylsulfonylierter Phenylalaninamide.