Study of Anti-Ischemic Effect of Afobazole in Experimental Myocardial Infarction

Kryzhanovskyi, S. A.; Сорокина, А. В.; Stolyaruck, V. N.; Вититнова, М. Б.; Мирошкина, И. А.; Цорин, И. Б.; Дурнев, А. Д.; Seredenin, S. B.

doi:10.1007/s10517-011-1131-4

Cited by 9 publications

(1 citation statement)

References 10 publications

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“…Previous pharmacological studies have identified ligand interaction of afobazole with MT 1 (K i = 1.6E-05 M), MT 3 (K i = 9.7E-07 M), r1 (SigmaR1) (K i = 5.9E-06 M) receptors and MAO A (K i = 3.6E-06 M) and defined its main effects as anxiolytic and neuroprotective . Further studies revealed its cardioprotective action (Stoliaruk et al 2010;Kryzhanovskyi et al 2011) and protective action in various toxicological models (Durnev et al 2009). These findings confirmed previously postulated hypothesis of cytoprotective potential of this anxiolytic drug ).…”

Section: Introductionmentioning

confidence: 99%

Contribution of Sigma‐1 receptor to cytoprotective effect of afobazole

Voronin

Kadnikov

2016

Pharmacol Res Perspect

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Anxiolytic afobazole (5‐Ethoxy‐2‐[2‐(morpholino)‐ethylthio]benzimidazole dihidrochloride) has pronounced ligand properties toward Sigma‐1 receptor (σ1 receptor,SigmaR1) and MT 3 receptors. Our previous work demonstrated that afobazole possess cytoprotective effect in the in vitro model of menadione genotoxicity (Woods et al. 1997) through interaction with MT 3 receptor (Kadnikov et al. 2014). Present study utilized previously described models to address the contribution of SigmaR1 to cytoprotective action of afobazole. The reduction in afobazole cytoprotective effect observed after preincubation of cell suspension with selective SigmaR1 antagonist BD‐1047 revealed an important contribution of SigmaR1 in afobazole‐mediated effect. We confirmed our observation using selective SigmaR1 agonist PRE‐084. We conclude that pronounced cytoprotective effect of afobazole over PRE‐084 is likely achieved by additive SigmaR1 and MT 3‐mediated effects.

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Section: Introductionmentioning

confidence: 99%

Contribution of Sigma‐1 receptor to cytoprotective effect of afobazole

Voronin

Kadnikov

2016

Pharmacol Res Perspect

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Delayed Results of Experimental Afobazole Therapy in Rats after Acute Myocardial Infarction

et al. 2017

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Delayed cardioprotective effects of anxiolytic Afobazole (15 mg/kg, intraperitoneally for 14 days) were evaluated using dynamic echocardiographic recordings on days 2, 15, 56, and 98 after experimental myocardial infarction modeling (rat model of acute myocardial ischemia). The cardiotropic activity of Afobazole is assumed to be related to its agonistic effects on σ receptor of cardiomyocytes. It was found that animals treated with Afobazole had no signs of heart failure by the end of observation, as evidenced by left ventricular ejection fraction.

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On the Mechanism of the Cardioprotective Action of σ1 Receptor Agonist Anxiolytic Fabomotizole Hydrochloride (Afobazole)

et al. 2018

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Original translational rat model of chronic heart failure provoked by experimental anterior transmural myocardium infarction was employed to examine the preventive action of anxiolytic Afobazole (15 mg/kg/day administered intraperitoneally during the first 15 days after coronary occlusion) on the development of the heart failure assessed in 3 months after infarction. Afobazole prevented the development of pathologic remodeling of the myocardium, maintained its inotropic function, and decreased the plasma level of brain natriuretic peptide known as a biochemical marker of chronic heart failure. In the myocardium, Afobazole down-regulated overexpression of the genes induced in chronic heart failure and assessed by corresponding RNA levels, which code angiotensin (AT1A-R), vasopressin (V1A-R), and glucocorticoid (GR) receptors as well as Epac2 protein. The revealed biochemical changes are consistent with the data on cardioprotective action of Afobazole.

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Study of Anti-Ischemic Effect of Afobazole in Experimental Myocardial Infarction

Cited by 9 publications

References 10 publications

Contribution of Sigma‐1 receptor to cytoprotective effect of afobazole

Contribution of Sigma‐1 receptor to cytoprotective effect of afobazole

Delayed Results of Experimental Afobazole Therapy in Rats after Acute Myocardial Infarction

On the Mechanism of the Cardioprotective Action of σ1 Receptor Agonist Anxiolytic Fabomotizole Hydrochloride (Afobazole)

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