Effect of Mexidol and Nitroxymexidol on Phosphodiesterase Activity, Some Oxidation Processes, and Hypoxia Resistance

• Published in: Pharmaceutical chemistry journal 2014-10, Vol.48 (7), p.417-420
• Main Authors: Tat’yanenko, L. V., Dobrokhotova, O. V., Varfolomeev, V. N., Fadeev, M. A., Fedorov, B. S., Shtol’ko, V. N., Mishchenko, D. V.
• Format: Article
• Language: English
• Subjects: Lipid peroxidation; Medicine; Molecular-Biological Problems of Drug Design and Mechanism of Drug Action; Organic Chemistry; Pharmacology/Toxicology; Pharmacy
• ISSN: 0091-150X; 1573-9031
• DOI: 10.1007/s11094-014-1123-6

The effect of mexidol (M) and nitroxymexidol (NM) on the activity of phosphodiesterase of cyclic guanosine monophosphate (PDEcGMP), regulation of lipid peroxidation (LPO), and antiradical and antihypoxic activity was investigated under normoxia and normobaric hypercapnic hypoxia conditions. Reversible and noncompetitive inhibition of the hydrolytic function of PDEcGMP by M and NM was revealed. The K i value for M was 1 ×10 –4 M; for NM, 1 ×10 –5 M, i.e., NM was 10 times more active than M. It was shown that the lifetime of experimental animals in a closed space increased by 36% under the action of M as compared with that of the control group while it increased by 53% for NM. The ventricular contraction time increased by 137% for NM. The atrial contraction time increased from 31 min in the control to 52 and 57 min for M and NM, respectively.