Medicinal Chemical Studies on Antiplasmin Drugs. I. Establishment of the Screening Assay Method for Antiplasmin Drugs and the Superiority of trans-4-Aminomethylcyclohexanecarboxylic Acid (Tranexamic Acid) to cis-Form

Abstract

The new caseinolytic assay method for antiplasmin activity of synthetic compounds was established by introducing the determination of ID₅0. trans-Form isomer of 4-aminomethylcyclohexanecarboxylic acid (tranexamic acid) was shown to have very potent antiplasmin activity whereas the cis-form isomer was little effective. The antiplasmin activity of tranexamic acid was 5-7 times greater than that of ε-aminocaproic acid.