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RUC-4: a novel αIIbβ3 antagonist for prehospital therapy of myocardial infarction.


ABSTRACT:

Objective

Treatment of myocardial infarction within the first 1 to 2 hours with a thrombolytic agent, percutaneous coronary intervention, or an αIIbβ3 antagonist decreases mortality and the later development of heart failure. We previously reported on a novel small molecule αIIbβ3 antagonist, RUC-2, that has a unique mechanism of action. We have now developed a more potent and more soluble congener of RUC-2, RUC-4, designed to be easily administered intramuscularly by autoinjector to facilitate its use in the prehospital setting. Here, we report the properties of RUC-4 and the antiplatelet and antithrombotic effects of RUC-2 and RUC-4 in animal models.

Approach and results

RUC-4 was ≈ 20% more potent than RUC-2 in inhibiting human ADP-induced platelet aggregation and much mo

SUBMITTER: Li J 

PROVIDER: S-EPMC4180209 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature