Pleyotropic antiaggregant effects of an innovative antiarrhythmic of class III SS-68, an indole derivative

Authors

  • Saida Kazbekovna Bogus Kuban State Medical University
  • Aleksandr Sergeevich Dukhanin Russian National Research Medical University named after N.I. Pirogov
  • Aida Fatihovna Kucheryavenko Volgograd State Medical University
  • Dmitry Vitalevich Vinakov Belgorod State University
  • Konstantin Phillipovich Suzdalev Southern Federal University
  • Pavel Alexandrovich Galenko-Yaroshevsky Kuban State Medical University

Abstract

Background: A new indole derivative with the lab code-number SS-68 demonstrates a   significant antiarrhythmic (anti-fibrillation) activity associated with the predominant influence on   potassium and calcium conductivity of cardiomyocytes plasmalemmas. The preliminary data give   evidence of SS-68 possessing an antiaggregant activity.

Methods: The influence of SS-68 on the platelet formation stage of hemostasis was determined   by assessment of the anti-platelet effect (measuring platelet aggregation with Born/ O’Brien   method), the dynamics of intracellular concentration of calcium ions in platelets was studied with   FURA-2/АМ fluorescent probe.

Results: Relative efficiency of the SS-68 indole derivative influence on platelet aggregation with   the use of various inducers decreases in the following order: collagen > serotonin > ADP. The   influence of SS-68 on platelet activity is characterized by pleiotropic effects: calcium-blocking   effect, potentiation of cAMP-response, suppression of intracellular mechanisms of transmitting a   stimulating signal, caused by the activation of collagen receptors.

Conclusion: G-proteins are the most likely molecular targets of pleiotropic antiaggregant effect   of SS-68. A more than threefold increase in the anti-platelet effect of SS-68 in vivo suggests the   development of an active metabolite (metabolites).  

Keywords:

SS-68 compound, platelet aggregation, disaggregation, intracellular calcium, molecular targets of anti-platelet effect

Author Contribution

Saida Kazbekovna Bogus, Kuban State Medical University

Candidate of Medical Sciences, Assistance Lecturer, Department of Pharmacology

Aleksandr Sergeevich Dukhanin, Russian National Research Medical University named after N.I. Pirogov

Holder of Habilitation Degree in Medicine, Professor, Department of Molecular Pharmacology and Radiobiology

Aida Fatihovna Kucheryavenko, Volgograd State Medical University

Holder of Habilitation Degree in Medicine, Associate Professor, Department of Pharmacology

Dmitry Vitalevich Vinakov, Belgorod State University

PhD Candidate, Department of Pharmacology

Konstantin Phillipovich Suzdalev, Southern Federal University

Candidate of Chemical Sciences, Associate Professor, Department of Chemistry of Natural and High-molecular Compounds, Faculty of Chemistry

Pavel Alexandrovich Galenko-Yaroshevsky, Kuban State Medical University

Corresponding Member of the Russian Academy of Sciences, Holder of Habilitation Degree in Medicine, Professor, Head of the Department of Pharmacology

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Published

30-06-2017

How to Cite

Bogus SK, Dukhanin AS, Kucheryavenko AF, Vinakov DV, Suzdalev KP, Galenko-Yaroshevsky PA (2017) Pleyotropic antiaggregant effects of an innovative antiarrhythmic of class III SS-68, an indole derivative. Research Results in Pharmacology 3(2): 3–13

Issue

Vol. 3 No. 2 (2017)

Section

Experimental Pharmacology

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