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

Abstract

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.