N-alkenylimidazole metal complex derivatives as effective agents for the hypoxic conditions

The therapy of hypoxemic conditions by the substances, which are differing because of their key role in the vital processes of metabolism and also their high pharmacological activity, and which are known to be the regulators of redox systems, can be considered as one of the priority directions of the modern clinical and experimental pharmacology. Metal complexes of essential elements, which are the natural participants of the ligand formation, can be very interesting in this sense. The research goal. Experimental validation of the pharmacological correction of the hypoxic conditions of the N-alkenyl-, Npropargylimidazoles and 3-hydroxypyridine metal complex derivative

Dermatoprotective activity of a combination of enoxifol with rexod in a reduced form the blood circulation in the skin in diabetes mellitus and hypercholesterinemia

Experiments in rats showed that the 9-diethylaminoethyl-2-(3,4-dioxyphenyl)-imidazo- [1,2-a]-benzimidazole dihydrobromide with the provisional name of enoxifol (0.94 - 15 mg/kg), rexod (recombinant human superoxide dismutase; 0.002 mg/kg) and especially their combination in intravenous administration in a reduced blood circulation in the skin against the background of the normoglycemia and hyperglycemia induced by experimental (alloxanic) diabetes mellitus complicated by exogenous hypercholesterinemia have a pronounced dose-dependent dermatoprotective effect, which may be due to the activation of energy processes and increase the reserve capacity of the antioxidant support network and normalization of carbohydrate and lipid metabolis

Anticholinergic activity and pharmacokinetic parameters of agent SS-68 with properties of class III antiarrhythmic drugs

It was shown that the indole derivate SS-68 (50 and 250 μg/kg intravenous) in acute experiments on cats with neurogenic atrial fibrillation (AF) has a dose-dependent antiarrhythmic action which is associated with the neurotropic influence of this substance, since the suppression of the AF coincides with its anticholinergic effect observed for more than 2 hours, but cardiotropic action at this time was not observed. High antiarrhythmic activity of SS-68 to neurogenic AF may be due to the IKAch inhibition and blockade of M2-cholinergic receptor

PHARMACOKINETIC RESEARCH OF POTENTIAL HYGOGLICEMIC DRUGS С7070

Introduction: The development of effective drugs for the treatment of diabetes is one of the urgent problems of modern medicine; we conducted pharmacokinetic studies of the innovative hypoglycemic drug - C7070, in rabbits and rats. Materials and Methods: The object of the study was substance C7070. Two methods of administration have been studied: intravenously and intragastrically. The concentration of C7070 is determined in blood plasma by a sensitive and selective HPLC method with tandem mass spectrometry detection. The range of detection was from 0.02 μg to 3876.00 μg in 1 ml of plasma in the animals under study. Chromatographic separation was performed on a 150 × 3.0 mm column of Zorbax Eclipce XDB C18 with a particle size of 3.0 μm (Agilent technologies, USA). To obtain stable results, a Zorbax Eclipce XDB C18 (Agilent technologies, USA) protection column of 12.5 × 3.0 mm with a particle size of 5.0 μm was used at 40 ° C for all analytical cycles. Ballast proteins in the test solutions were precipitated with acetonitrile followed by extraction of the analyte with ultrasound. Results and its Discussion: With intragastric administration, the maximum concentration (Cmax) of C7070 in blood plasma reached, on average, in rabbits through (tmax) 60 ± 0.1 minutes, in rats after 170.0 ± 79.8 minutes and was 34.6 ± 7.3 μg/ml and 17.6 ± 1.4 μg/ml, respectively. The half-life (t1/2) was prolonged and was 291.8 ± 17.1 minutes for rabbits and 225.2 ± 12.4 minutes for rats. The absolute bioavailability (fa) of C7070 in rabbits was 78.2 ± 1.0%, in rats 18.1 ± 2.0%. When administered intravenously, Cmax C7070 in blood plasma averaged 123.1 ± 23.7 μg/ml in rabbits and 337.6 ± 40.5 μg/ml in rats. The half-life period (t1/2) was prolonged and amounted to 225.5 ± 15.9 minutes for rabbits and 154.1 ± 5.1 minutes for rats. The Conclusion: The pharmacokinetic characteristics of a potential hypoglycemic drug C7070 in animals (rats, rabbits) under two routes of administration, intra-gastrointestinal and intravenous, were studied. The parameters obtained can be useful for clinical application and further studies of C7070 drugs based on it. Key words: C7070, diabetes mellitus, hypoglycemic agents, blood plasma of rabbits and rats, high-performance liquid chromatography, pharmacokinetics

Phugoid motion for grazing-entry trajectories at near-circular speeds

Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/77023/1/AIAA-26742-801.pd

N-alkenylimidazole metal complex derivatives as effective agents for the hypoxic conditions

The therapy of hypoxemic conditions by the substances, which are differing because of their key role in the vital processes of metabolism and also their high pharmacological activity, and which are known to be the regulators of redox systems, can be considered as one of the priority directions of the modern clinical and experimental pharmacology. Metal complexes of essential elements, which are the natural participants of the ligand formation, can be very interesting in this sense. The research goal. Experimental validation of the pharmacological correction of the hypoxic conditions of the N-alkenyl-, Npropargylimidazoles and 3-hydroxypyridine metal complex derivative