Study of analeptic activity of tetrahydropyrido [2,1-b] [1,3,5] tiadiazine derivatives

Авторы

  • Elena Yu. Bibik SI "Lugansk State Medical University the name of St. Luke"
  • Anna A. Saphonova SI "Lugansk State Medical University the name of St. Luke"
  • Anton V. Yeryomin SI "Lugansk State Medical University the name of St. Luke"
  • Konstantin A. Frolov SI "Lugansk State Medical University the name of St. Luke"; Research Institute "Himeх" GOU VPO "Lugansk State University
  • Victor V. Dotsenko Research Institute "Himeх" GOU VPO "Lugansk State University; FGBOU HPE "Kuban State University"
  • Sergey G. Krivokolysko SI "Lugansk State Medical University the name of St. Luke"; 2Research Institute "Himeх" GOU VPO "Lugansk State University

DOI:

https://doi.org/10.18413/2313-8971-2017-3-4-20-25

Аннотация

Introduction: Our goal is to conduct an investigation of the analeptic activity of the tetrahydropyrido [2,1-b] [1, 3, 5] thiadiazine derivative group.

Materials and Methods: Biological studies were carried out on 78 white pedigreed mature sexually transmitted rats of both sexes weighing 230-270 g in the autumn-winter period. The test substances were administered intragastrically at a dose of 5 mg/kg 1 hour prior to the induction of anesthesia. Animals of the control group received thiopental sodium at a dose of 70 mg/kg. As the reference preparation, sodium caffeinebenzoate was used intraperitoneally at a dose of 10 mg/kg.

Results and Discussion: In the group of experimental animals that received intragastric substance 1 1 hour before thiopental anesthesia, a six-fold prolongation of the period of injection into anesthesia was found, the duration of anesthesia was comparable to that of the control. However, after 16 hours, 33.3% of the rats died, the rest of the animals were sharply inhibited. The original substance with laboratory cipher 2 significantly increases the time of introduction into anesthesia, has a pronounced analeptic activity, superior to that of caffeine.

Conclusion: Thus, the conducted studies on the presence of 10 new biologically active compounds based on tetrahydropyrido [2,1-b] [1, 3, 5] thiadiazine derivatives in the spectrum of pharmacological activity showed the presence of the most pronounced analeptic and antinarcotic activity in compounds with laboratory ciphers 3, 6, 7 and 10. Compound 2, which is 6-oxo-8- {4 – [(2-chlorobenzyl) oxy] phenyl} -3- (2- ethoxyphenyl) -3,4,7,8-tetrahydro -2H, 6H-pyrido [2,1-b] [1, 3, 5] thiadiazine-9- carbonitrile, the analeptic effect is significantly superior to that of caffeine-benzoate that of sodium.

Ключевые слова:

analeptic activity, derivatives of tetrahydropyrido[2,1-b][1,3,5]thiadiazine, thiopental sodium, caffein-sodium benzoate

Вклад авторов

Elena Yu. Bibik, SI "Lugansk State Medical University the name of St. Luke"

Doctor of Medical Sciences, Head of the Department of Fundamental and Clinical Pharmacology.

Anna A. Saphonova, SI "Lugansk State Medical University the name of St. Luke"

Assistant of the Department of Fundamental and Clinical Pharmacology.

Anton V. Yeryomin, SI "Lugansk State Medical University the name of St. Luke"

Candidate of Sciences, Associative professor of the Department of Fundamental and Clinical Pharmacology.

Konstantin A. Frolov, SI "Lugansk State Medical University the name of St. Luke"; Research Institute "Himeх" GOU VPO "Lugansk State University

Assistant of the Department of Pharmaceutical Chemistry and Pharmacognosy; PhD in Chemistry, Leading Engineer.

Victor V. Dotsenko, Research Institute "Himeх" GOU VPO "Lugansk State University; FGBOU HPE "Kuban State University"

Doctor of Chemical Sciences, Leading Researcher; Associate Professor of the Department of Organic Chemistry and Technologies.

Sergey G. Krivokolysko, SI "Lugansk State Medical University the name of St. Luke"; 2Research Institute "Himeх" GOU VPO "Lugansk State University

Doctor of Chemical Sciences, Scientific Leader; Head of the Department of Pharmaceutical Chemistry and Pharmacognosy.

Загрузки

Опубликован

30.12.2017

Как цитировать

Bibik EY, Saphonova AA, Yeryomin AV, Frolov KA, Dotsenko VV, Krivokolysko SG (2017) Study of analeptic activity of tetrahydropyrido [2,1-b] [1,3,5] tiadiazine derivatives. Research Results in Pharmacology 3(4): 20–25. https://doi.org/10.18413/2313-8971-2017-3-4-20-25

Выпуск

Раздел

Экспериментальная фармакология

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