PRECLINICAL FINDINGS OF NEW CYCLOHEXILAMMONIUM SALT 2-[1-ETHYL-3-METHYL-7-(DIOXOTHIETANYL-3)XANTHINYL- 8-THIO]ACETIC ACID WITH RESPECT TO HEMOSTASIS SYSTEM UNDER CONDITIONS IN VITRO
Issue:
8
Year:
2016
The paper shows preclinical findings of new cyclohexilammonium salt 2-[1-ethyl-3-methyl-7-(dioxothietanyl-3)xanthinyl-8-thio]acetic acid
under intraperitoneal injection in rats and its comparison with analog product of pentoxifylline. The impact of firstly synthesized derivative xantine
and pentoxifylline on the functional activity of platelets under conditions in vivo was studied with the help of a laser analyzer of platelet aggregation
Biola 230 LA (Russia). Adenosinediphosphate, collagen, epinephrine and ristocetin were used as an aggregation inducer. Aggregatograms were
analyzed with the help of AGGR software. Thromboelastography (TEG 5000, Haemoscope Corporation, USA) was performed in accordance with instructions
of the manufacture and performed within 1 h of blood sampling. Thromboelastography parameters of reaction time, angle and maximal
amplitude and conventional coagulation data of platelet count. Activity of factor 3 platelets was defined in accordance with the V. Rabiner method.
Definition of factor 4 platelets was carried out under the effect that heated plasma poor in platelets exerts on thrombin-heparin time of plasma coagulation
according to the L.A. Matviyenko and M.A. Kotovschikaya method. Release of P3 и P4 factors during platelet aggregation was appraised after
aggregation carried out by adenosinediphosphate and centrifugation. The research has determined that new cyclohexilammonium salt is exceeds
pentoxifylline spectrumwise and levelwise in terms of antiaggregational activity. The findings show the absence of the second wave of
platelet aggregation induced by small doses of ADP, prolongation of lag-period under collagen-induced platelet aggregation as well as the reduced
availability and release of platelet factors 3 and 4 which proves the affect of new cyclohexilammonium salt 2-[1-ethyl-3-methyl-7-(dioxothietanyl-
3)xanthinyl-8-thio]acetic acid as a potential inhibitor of platelet release reaction.
Keywords:
Key words: 1-ethylxanthine derivatives
hemostasis
antiaggregation activity
platelet release reaction.