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

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

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 wa...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1968/02/25, Vol.16(2), pp.357-363
Hauptverfasser: SHIMIZU, MASAO, AOYAGI, TAKAAKI, IWAMOTO, MASAHIRO, ABIKO, YASUSHI, NAITO, TAKEO, OKANO, ATSUJI
Format: Artikel
Sprache:eng
Schlagworte:
Caseins
Cyclohexanecarboxylic Acids - pharmacology
Fibrinolysin - antagonists & inhibitors
Humans
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Zusammenfassung: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.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.16.357