Эндотелио- и кардиопротекторное действие в ряду производных 3-(2,2,2-триметилгидразиний) пропионата
2012
The article presents the results of studies on endothelial and cardioprotective activity of 3-(2,2,2-trimetilgidraziny) propionate and its derivatives. Found that 3-(2,2,2-trimetilgidraziny) propionate at a dose of 90 mg / kg and its derivatives (nicotinate -189.0 mg / kg, 5-bromnikotinat 237.3 mg / kg, 5-gidroksinikotinat-199, 1 mg / kg, glycinate-159, 6 mg / kg) 3-(2,2,2-trimetilgidraziny) propionate potassium, have a marked endothelial and cardioprotective effects on the model of L-NAME-induced nitric oxide deficiency in rats, which is expressed the predominance of endothelium-dependent relaxation of blood vessels and reducing the rate of endothelial dysfunction to the level of the range of 1.6-2.1 and 2.8 derived from the 3-(2,2,2-trimetilgidraziniya) propionate, the positive dynamics of the results of stress tests. We also show that the introduction to the molecular structure of 3-(2,2,2-trimetilgidraziny) propionate new functional groups, such as a nicotinic acid, which lipid-lowering and vasoactive properties are well known, leads to increased endothelial and cardioprotective activity of the studied substances. Set the most pronounced endothelial and cardioprotective effects among the derivatives of 3-(2,2,2-trimetilgidraziniya) propionate was established in 5-gidroxynicotinat, which manifests itself in the maximum reduction factor of endothelial dysfunction and positive stress tests results.
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