4.4 Article

The antithrombotic and haemostatic effects of LASSBio-752: a synthetic, orally active compound in an arterial and venous thrombosis model in rats

Journal

JOURNAL OF PHARMACY AND PHARMACOLOGY
Volume 69, Issue 10, Pages 1374-1380

Publisher

WILEY
DOI: 10.1111/jphp.12771

Keywords

acylhydrazones; antiplatelet drugs; PAR; platelet; thrombosis

Funding

  1. CAPES
  2. CNPq
  3. FAPERJ
  4. CT-INFRA-FINEP

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ObjectivesIn this work, we further investigated the effect of the compound LASSBio-752 in thrombosis models in rats. MethodsArterial and venous thrombosis model, ex-vivo recalcification time and aPTT and PT. Key findingsIn the venous thrombosis model, oral administration of LASSBio-752 [48.2 mg (100 mol)/kg] one hour before the thrombus induction decreased thrombus weight by 37 0.2%. Interestingly, the antithrombotic action of this compound [48.2 mg (100 mol)/kg] occurred at 87.5 +/- 2.1% of inhibition after 24 h of administration and showed a lasting activity. When tested on the arterial thrombosis model, after a 1-h interval, there was already an increase in time to total occlusion of 34 +/- 2.4 min, but the greatest effect was observed at intervals between 6 and 15 h of administration, when no occlusion of the artery was observed. The antithrombotic effect was reduced after 24 h when the occlusion time was 23.8 +/- 2.3 min, close to that of the control, 17.6 +/- 2.0 min. We also observed that bleeding was not excessive in any of the intervals tested. ConclusionsOur results indicate that compound LASSBio-752 is a potential candidate for utilization in the treatment of thromboembolic diseases.

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