title: Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide.
abstract: Substituted thiadiazines exert a reliable therapeutic effect in treating stress, and a schematic description of their ability to influence all aspects of a stress response has been depicted. This study was conducted to pharmacologically evaluate compound L-17, a substituted thiadiazine, (2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide) for possible anti-psychotic/antidepressant activity. Compound L-17 was synthesized by cyclocondensation of α-bromoacetophenone with the original morpholine-4-carbothionic acid hydrazide. Pharmacologic evaluations were conducted using methods described by E.F. Lavretskaya (1985), and in accordance with published guidelines for studying drugs for neuroleptic activity. Compound L-17 was evaluated for various possible mechanisms of action, including its effects on cholinergic system agonists/antagonists, dopaminergic neurotransmission, the adrenergic system, and 5-HT3 serotonin receptors. One or more of these mechanisms may be responsible for the beneficial effects shown by thiadiazine compounds in experiments conducted to evaluate their activity in models of acute stress and acute myocardial infarction.
authors.affiliation: Ural Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, Russia. a.sarapultsev@gmail.com.|Institute of Immunology and Physiology of the Ural Branch of the RAS, Ekaterinburg 620219, Russia. a.sarapultsev@gmail.com.
authors.forename: Alexey P
authors.initials: AP
authors.lastname: Sarapultsev
authors.affiliation: Ural Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, Russia. chupakhin@ios.uran.ru.|The IJ Postovsky Institute of Organic Synthesis of the Ural Branch of the RAS, Ekaterinburg 620990, Russia. chupakhin@ios.uran.ru.
authors.forename: Oleg N
authors.initials: ON
authors.lastname: Chupakhin
authors.affiliation: Ural Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, Russia. p.sarapultsev@gmail.com.|Institute of Immunology and Physiology of the Ural Branch of the RAS, Ekaterinburg 620219, Russia. p.sarapultsev@gmail.com.
authors.forename: Petr A
authors.initials: PA
authors.lastname: Sarapultsev
authors.affiliation: Ural Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, Russia. vlapp@isnet.ru.
authors.forename: Larisa P
authors.initials: LP
authors.lastname: Sidorova
authors.affiliation: Ural Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, Russia. tseitler85@mail.ru.
authors.forename: Tatiana A
authors.initials: TA
authors.lastname: Tseitler
keywords: 1,3,4-thiadiazine-2-amines; adrenoblockers; heterocycles; pharmacological evaluation; serotonin; stress; thiadiazines; α-adrenoblockers