RESUMEN
Experiments in vitro with the use of a rat brain homogenate demonstrated antioxidant activity of methyl ether (3(2,2,2-trimethylhydrazinium) propionate possessing a positive charge at the quaternary nitrogen atom. The antioxidant activity was due to intensified neutralization of superoxide anion radicals and, correspondingly, inhibited peroxidation of endogenous brain lipids. The other compounds under study, namely, gamma-butyrobetaine, its methyl ether, and 3(2,2,2-trimethylhydrazine) propionate did not exhibit antioxidant properties.
Asunto(s)
Betaína/análogos & derivados , Encéfalo/efectos de los fármacos , Fármacos Cardiovasculares/farmacología , Carnitina , Peroxidación de Lípido/efectos de los fármacos , Metilhidrazinas/farmacología , Superóxidos/metabolismo , Animales , Betaína/farmacología , Encéfalo/metabolismo , Éteres , Técnicas In Vitro , Masculino , Malondialdehído/metabolismo , Metilhidrazinas/metabolismo , Oxidación-Reducción , Ratas , Relación Estructura-ActividadRESUMEN
Oral administration of mildronate, 3-(2,2,2-trimethylhydrazine)propionate, an inhibitor of carnitine-dependent metabolism, in a dose of 50-100 mg/kg for 10 days promoted a rapid restoration of contractility of Langendorf perfused rat heart preparations during postischemic perfusion and protected the rat hearts against inhibition of contractile function resulting from continuous perfusion with palmitic acid. Mildronate inhibits gamma-butyrobetaine hydroxylase, depresses carnitine biosynthesis and reduces carnitine-dependent fatty acid metabolism. The cardioprotective effect of mildronate is particularly manifest upon continuous administration.