Studying the adaptogenic activity of a series of tetrahydropyrido[2,1-b] [1,3,5] thiadiazine derivatives
https://doi.org/10.20538/1682-0363-2019-3-21-28
Abstract
Introduction. In the modern world people are exposed to the influence of adverse psychological and physical factors, escalating in intensity. The search for new pharmacodynamic effects of [1,3,5]-thiadiazine derivatives designated by significant biological activity of these compounds is an essential issue.
Aim. To research adaptogenic activity of tetrahydropyrido[2,1-b][1,3,5]thiadiazine derivatives using a modified Porsolt Forced Swim Test.
Materials and methods. Four substances from the group of 3-R-8-aryl-6-oxo-3,4,7,8-tetrahydro-2H,6Hpyrido[2,1-b][1,3,5]thiadiazine-9-carbonitriles were selected for the research. Rats were divided into a control group, 5 reference groups (amitriptyline, caffeine, thiotriazolin, thiocetam, ginseng) and 4 experimental groups according to the number of the studied original tetrahydropyrido[2,1-b][1,3,5] thiadiazine derivatives.
Results. Intragastric injection of substance 2 for 5 days in the modified forced swim test (forced swimming with freight) increased work capacity and endurance of the rats by 103.42% as opposed to the initial results. The detected adaptogenic activity of this tetrahydropyrido[2,1-b][1,3,5]thiadiazine derivative six times exceeds adaptogenic activity of ginseng and seven times that of amitriptyline. The rats in the control group were active for a bit longer time. Ginseng raised the time of activity by 17% at day 5. Caffeine essentially reduced work capacity and endurance. Amitriptyline showed adaptogenic activity at day 3 of the research (increase by 10.4%). Thiotriazolin also showed adaptogenic activity on day 3 of the research (increase by 30.17%). Thiocetam increased the time of activity by 78.55%. Substance 4 had adaptogenic activity too; it increased the time of activity in aversive conditions by 58.25%, which three times exceeds this parameter for ginseng and four times for amitriptyline.
About the Authors
E. Yu. Bibik
Lugansk State Medical University named after Saint Luka
Russian Federation
Russian Federation
DM, Professor, Head of the Department of Fundamental and Clinical Pharmacology,
1g, Sq. 50th Anniversary of the Defense of Lugansk 91045, Lugansk, Lugansk People’s Republic
I. A. Nekrasa
Lugansk State Medical University named after Saint Luka
Russian Federation
Russian Federation
Student,
1g, Sq. 50th Anniversary of the Defense of Lugansk 91045, Lugansk, Lugansk People’s Republic
A. V. Demenko
Lugansk State Medical University named after Saint Luka
Russian Federation
Russian Federation
V., PhD, Associate Professor, Department of Pharmaceutical Chemistry and Pharmacognosy,
1g, Sq. 50th Anniversary of the Defense of Lugansk 91045, Lugansk, Lugansk People’s Republic
K. A. Frolov
Lugansk State Medical University named after Saint Luka;
Lugansk National University named after Vladimir Dahl
Russian Federation
Russian Federation
PhD, Associate Professor, Department of Pharmaceutical Chemistry and Pharmacognosy, 1g, Sq. 50th Anniversary of the Defense of Lugansk 91045, Lugansk, Lugansk People’s Republic;
Build. 7, 20A, Sq. Molodezhnyj, 91034, Lugansk, Lugansk People’s Republic
V. V. Dotsenko
Lugansk National University named after Vladimir Dahl;
Kuban State University
Russian Federation
Russian Federation
Head of the Department of Organic Chemistry and Technologies, Build. 7, 20A, Sq. Molodezhnyj, 91034, Lugansk, Lugansk People’s Republic;
DСhSc, Professor, 149, Stavropolskaya Str., 350040, Krasnodar
S. G. Krivokolysko
Lugansk State Medical University named after Saint Luka;
Lugansk National University named after Vladimir Dahl
Russian Federation
Russian Federation
DСhSc, Professor, Head of the Department of Pharmaceutical Chemistry and Pharmacognosy, 1g, Sq. 50th Anniversary of the Defense of Lugansk 91045, Lugansk, Lugansk People’s Republic;
Build. 7, 20A, Sq. Molodezhnyj, 91034, Lugansk, Lugansk People’s Republic
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Review
For citations:
Bibik E.Yu., Nekrasa I.A., Demenko A.V., Frolov K.A., Dotsenko V.V., Krivokolysko S.G. Studying the adaptogenic activity of a series of tetrahydropyrido[2,1-b] [1,3,5] thiadiazine derivatives. Bulletin of Siberian Medicine. 2019;18(3):21-28. (In Russ.) https://doi.org/10.20538/1682-0363-2019-3-21-28
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