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The antithrombotic and haemostatic effects of LASSBio-752: a synthetic, orally active compound in an arterial and venous thrombosis model in rats.
Frattani, Flávia S; Lima, Lidia M; Barreiro, Eliezer J; Zingali, Russolina B.
Afiliación
  • Frattani FS; Laboratório de Hemostasia e Trombose - LHT, Departamento de Análises Clínicas e Toxicológicas - DACT, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro - UFRJ, Rio de Janeiro, RJ, Brazil.
  • Lima LM; Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®), ICB-CCS, Cidade Universitária, Universidade Federal do Rio de Janeiro - UFRJ, Rio de Janeiro, RJ, Brazil.
  • Barreiro EJ; Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio®), ICB-CCS, Cidade Universitária, Universidade Federal do Rio de Janeiro - UFRJ, Rio de Janeiro, RJ, Brazil.
  • Zingali RB; Instituto de Bioquímica Médica-CCS- UFRJ, Rio de Janeiro, RJ, Brazil.
J Pharm Pharmacol ; 69(10): 1374-1380, 2017 Oct.
Article en En | MEDLINE | ID: mdl-28722151
ABSTRACT

OBJECTIVES:

In this work, we further investigated the effect of the compound LASSBio-752 in thrombosis models in rats.

METHODS:

Arterial and venous thrombosis model, ex-vivo recalcification time and aPTT and PT. KEY

FINDINGS:

In the venous thrombosis model, oral administration of LASSBio-752 [48.2 mg (100 µmol)/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 µmol)/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.

CONCLUSIONS:

Our results indicate that compound LASSBio-752 is a potential candidate for utilization in the treatment of thromboembolic diseases.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Hemostáticos / Enfermedades de las Arterias Carótidas / Trombosis de la Vena / Fibrinolíticos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: J Pharm Pharmacol Año: 2017 Tipo del documento: Article País de afiliación: Brasil

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Hemostáticos / Enfermedades de las Arterias Carótidas / Trombosis de la Vena / Fibrinolíticos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: J Pharm Pharmacol Año: 2017 Tipo del documento: Article País de afiliación: Brasil