V. G. Zin'kovskii

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A study was made of the time course of alterations in the convulsant activity of corazol after injection to mice of 1,4-benzodiazepine derivatives with different chemical structure. Significant anticonvulsant effect of benzodiazepines was observed for 5--120 minutes and was regarded a dynamic index. The maximal action of the drugs was observed within 15--30(More)
Excretion of phenazepam and its metabolites in the bile and its intrahepatic circulation were studied in two groups of rats: bile donors receiving an intravenous injection of14C-phenazepam (14 mg/kg) previously, and recipients into whose duodenum the donors' bile was introduced. Phenazepam (compound I), its free-hydroxy metabolites (compound II), and a(More)
4. I. J. Czuczwar and B. Meldrum, Eur. J. Pharmacol., 83, 335-338 (1982). 5. P. R. Dodd, H. F. Bradford, A. S. Abdul-Ghani, et al., Brain Res., 193, 505-517 (1980). 6. R. H. Evans, A. A. Francis, A. W. Jones, et al., Br. J. Pharmacol., 75, 65-75 (1982). 7. Glutamate: Transmitter in the Central Nervous System, Chichester (1981). 8. R. L. Krall, J. K. Lenry,(More)
We studied the pharmacokinetics of 14C-ethanol administered in various doses and via different routes to CBA, C57Bl/6, and (CBA×C57Bl/6)F1 mice. Kinetic scheme of ethanol distribution included its elimination by enzymatic (80-90% C0) and exponential (10-20% C0) mechanisms. Ethanol pharmacokinetics did not depend on the administration route and mouse strain.(More)
In comparison with the literature data the pharmacological effects of muscimol (MS) on mice organism were studied under the condition of administration of the exogenic ligands of GABA-receptor complex GABA antagonist bicuculline (BC), chloride ionophor blocking agent pentylenetetrazole (PZ), phenazepam (BD), sodium barbital (BB) and GABA synthesis(More)
The types of the interaction of the pharmacological effects of ethanol and barbiturate antagonists--picrotoxin, bemegride and corasol--were determined. The effect of ethanol was determined as competitive--for the convulsant effects of bicuculline, and non-competitive--for the effects of thiosemicarbazide. The indices of the anticonvulsant effects of(More)
i. R. Ya. Al'tshuler, New Drug Preparations [in Russian], No. 3 (1976), pp. 13-19. 2. V. ~.~Zakusov, Khim.-farm. Zh., 13, No. i0, 108-112 (1979). 3. L.M. Filippova, I. A. Rapoport, Yu. L. Shapiro, et al., Genetika, Ii, No. 6, 77-79 (1975). 4. S.B. Seredenin, A. A. Vedernikov, and A. D. Durnev, Paper deposited at the All-Union Institute of Scientific and(More)
In the preceding papers [1-3], we showed that phenazepam [7-bromo-5-(o-chlorophenyl)l ,2-dihydro3H-1,4-benzdiazepin-2-one] (I) has a high physiological activity, and in several tests exceeds certain preparations of the 1,4-benzdiazepine series . To study the metabolism and pharmacokinetics, and to clarify certain aspects of the action mechanism of I, we(More)
The alternative and graduated methods for estimation of fast-reversible effects of ethanol are compared. Estimation of the myorelaxing and anticonvulsive effects of ethanol by the alternative method can be used with some limitations for the effector analysis of ethanol pharmacokinetics. It is shown that the effector expectation of pharmacokinetic profile(More)
The pharmacokinetics of 1,4-benzodiazepine derivatives has now been adequately studied. However, no data generalizing these resultsand indicating similarity or difference between the metabolic pathways or kinetics of distribut&on of preparations of the 1,4-benzodiazepine series are yet available. There are several reasons for this. First, these preparations(More)