Features of hemostatic activity of 2-[3-methyl-1-h-propyl-7-(1,1-dioxothiethanyl-3) xantinyl-8-thio] acetic acid cyclohexilammonium salt
- Authors: Kamilov FK.1, Timirkhanova GA1, Samorodova AI1, Khaliullin FA1, Gubaeva RA1
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Affiliations:
- Bashkir State Medical University, Ufa, Russia
- Issue: Vol 94, No 4 (2013)
- Pages: 549-552
- Section: Experimental medicine
- URL: https://bakhtiniada.ru/kazanmedj/article/view/1969
- DOI: https://doi.org/10.17816/KMJ1969
- ID: 1969
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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.
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##article.viewOnOriginalSite##About the authors
F Kh Kamilov
Bashkir State Medical University, Ufa, Russia
G A Timirkhanova
Bashkir State Medical University, Ufa, Russia
A I Samorodova
Bashkir State Medical University, Ufa, Russia
Email: avsamorodov@gmail.com
F A Khaliullin
Bashkir State Medical University, Ufa, Russia
R A Gubaeva
Bashkir State Medical University, Ufa, Russia
References
- Камилов Ф.Х., Тимирханова Г.А., Самородова А.И. и др. Поиск активных соединений среди производных 2-[3-метил-1-этил-7-(диоксотиетанил-3)ксантинил-8-тио] уксусной кислоты, влияющих на систему гемостаза // Фундамент. исслед. - 2011. - №9. - С. 254-256.
- Камилов Ф.Х., Тимирханова Г.А., Самородов А.В. и др. Соли [3-метил-1-н-пропил-7-(1,1-диоксотиетанил-3)ксантинил-8-тио] уксусной кислоты, проявляющие проагрегантную активность. Патент на изобретение №2459825. Бюлл. №24 от 27.08.2012.
- Руководство по экспериментальному (доклиническому) изучению новых фармакологических веществ / Под общ. ред. Р.У. Хабриева. - М.: Медицина, 2005. - 327 с.
- Воrn G.V. Aggregation of blood platelets by adenosine diphosphate and its reversal // Nature. - 1962. - Vоl. 194. - Р. 927-929.
- Elbourne D.S. Randomised controlled trial of prophylactic etamsylate: follow up at 2 years of age // NY Acad. Sci. - 1987. - Vol. 205. - P. 9-13.
- Gabbasov Z.A. The use of optical density fluctuations for determination of platelet concentration in stirred suspension // Platelets. - 1992. - Vol. 3. - P. 281-282.
- Keith I. Ethamsylate and blood loss in total hip replacement // Anaesthesia. - 1979. - Vol. 34, N 7. - P. 666-670.
- Schulte J., Osborne J., Benson J.W. et al. Developmental outcome of the use of etamsylate for prevention of periventricular haemorrhage in a randomised controlled trial // Arch. Dis. Child Fetal. Neonatal. Ed. - 2005. - Vol. 90, N 1. - P. 31-35.
- Spahn D.R. Severe bleeding in surgical and trauma patients: the role of fibrinogen replacement therapy // Thromb. Res. - 2012. - Vol. 130, N 2. - P. 15-19.
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