Antithrombotic Activity of a New P2Y1 Receptor Antagonist, Substance Sbt-119, on Experimental Models of Thromboses in Rats

• Published in: Bulletin of experimental biology and medicine Vol. 158; no. 1; pp. 53 - 56
• Main Authors: Yakovlev, D. S., Spasov, A. A., Bukatina, T. M., Smirnov, A. V., Suzdalev, K. F.
• Format: Journal Article
• Language: English
• Published: Boston Springer US 01.11.2014
• Subjects: Administration, Oral; Animals; Animals, Outbred Strains; Biomedical and Life Sciences; Biomedicine; Cell Biology; Drug Evaluation, Preclinical; Fibrinolytic Agents - administration & dosage; Indoles - administration & dosage; Internal Medicine; Laboratory Medicine; Lung - pathology; Male; Mice; Morpholines - administration & dosage; Pathology; Purinergic P2Y Receptor Antagonists - administration & dosage; Rats; Thrombosis - drug therapy; Ticlopidine - pharmacology; ticlopidine; indole derivatives; arterial thrombosis; receptor antagonists; ADP-induced systemic thrombosis; P2Y
• ISSN: 0007-4888; 1573-8221
• DOI: 10.1007/s10517-014-2690-y

Antithrombotic properties of a new P2Y 1 receptor antagonist N-[(1-morpholinopropyl-amino)- carbonyl-2-(1-ethyl-1H-indole-3-yl)-vinyl]-4-methylphenyl-amide hydrochloride, substance Sbt-119, and reference drug ticlopidine were studied on experimental models of arterial and systemic thromboses. Substance Sbt-119 was 39.9% ( p <0.05) more potent than ticlopidine in producing the antithrombotic effect. Moreover, substance Sbt-119 was shown to increase the survival rate of animals after systemic treatment with ADP (by 20%, p <0.0001). This substance decreased the number of mural thrombi and reduced the severity of hemodynamics disturbances in the organs during systemic thrombosis.