The effects of Nothrombel on the thrombin-induced formation of thrombocyte-leukocyte complexes (TLC) were studied. Nothrombel was found to produce dose-dependent inhibition of TLC formation. Its activity was greater than that of reference drug aspirin. The 50% inhibition constant (EC50) of Nothrombel was 1.75 μmol/ml, compared with greater than 1.75 μmol/ml for aspirin. The mechanism of inhibition of TLC formation by Nothrombel relates to the ability of this drug to suppress the expression of P-selectin by thrombocytes and the membrane complex GPIb-IX-V on membranes and the mobilization of cytoplasmic calcium in thrombocytes, and, evidently, an inhibitory action on the P2Y12 purine receptors of thrombocytes.
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Translated from Rossiiskii Fiziologicheskii Zhurnal imeni I. M. Sechenova, Vol. 103, No. 3, pp. 318–326, March, 2017.
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Veselkina, O.S., Petrishchev, N.N., Vasina, L.V. et al. Effects of Nothrombel on Thrombin-Induced Formation of Thrombocyte-Leukocyte Complexes. Neurosci Behav Physi 48, 830–834 (2018). https://doi.org/10.1007/s11055-018-0636-y
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DOI: https://doi.org/10.1007/s11055-018-0636-y