Features of hemostatic activity of 2-[3-methyl-1-h-propyl-7-(1,1-dioxothiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt

Abstract

Aim. To study the systemic hemostatic activity of firstly synthesized 2-[3-methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt in vitro and in vivo. Methods. Experiments in vitro using the blood samples form healthy male donors, and in vivo on male rats by intraperitoneal injection of the equimolar concentrations of researched substances. The effect of the firstly synthesized xantine and etamsylate derivative on the platelet functional activity in vitro and in vivo was studied using a platelet aggregation laser analyzer «Biola 230 LA» (Russia). 20 mkg/ml of adenosinediphosphate and 5 mg/ml of collagen (produced by «Technologia-Standart» company, Russia) were used as an aggregation inducers. Aggregation was analyzed using the AGGR software. General aggregation parameters, maximal aggregation value, maximal aggregation speed, average size of platelet aggregates were analyzed. Experimental assessment of specific systemic hemostatic activity in vivo was made in accordance with the parenchymal hemorrhage model on mature male rats. Coagulation time and blood loss volume were registered. Results. 2-[3-Methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt showed a pro-aggregative effect both in vitro and in vivo. 2-[3-Methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt pro-aggregative effect which was observed both in vitro and in vivo increased the systemic hemostatic activity, exceeding the results of the control group and etamsylate group. Conclusion. The findings reveal potentially high systemic hemostatic activity of 2-[3-methyl-1-h-propyl-7-(1,1-dioxotiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt and confirm the need for further studies of this compound and its equivalents in order to create highly effective selective hemostasis correctors on their basis.

Keywords

xantine derivatives / hemostatic system / pro-aggregate activity / hemostatic activity

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RIGHTS & PERMISSIONS

Kamilov F.K., Timirkhanova G.A., Samorodova A.I., Khaliullin F.A., Gubaeva R.A.