Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide
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-morpholin...
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MDPI AG
2016-05-01
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| Series: | Pharmaceuticals |
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| Online Access: | http://www.mdpi.com/1424-8247/9/2/27 |
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| author | Alexey P. Sarapultsev Oleg N. Chupakhin Petr A. Sarapultsev Larisa P. Sidorova Tatiana A. Tseitler |
| author_facet | Alexey P. Sarapultsev Oleg N. Chupakhin Petr A. Sarapultsev Larisa P. Sidorova Tatiana A. Tseitler |
| author_sort | Alexey P. Sarapultsev |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-11T10:33:45Z |
| format | Article |
| id | doaj.art-42cc8c1a767d4164a66abc30182c39eb |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-12-11T10:33:45Z |
| publishDate | 2016-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-42cc8c1a767d4164a66abc30182c39eb2022-12-22T01:10:48ZengMDPI AGPharmaceuticals1424-82472016-05-01922710.3390/ph9020027ph9020027Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine HydrobromideAlexey P. Sarapultsev0Oleg N. Chupakhin1Petr A. Sarapultsev2Larisa P. Sidorova3Tatiana A. Tseitler4Ural Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, RussiaUral Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, RussiaUral Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, RussiaUral Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, RussiaUral Federal University named after the first President of Russia B. N. Yeltsin, Ekaterinburg 620002, RussiaSubstituted 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.http://www.mdpi.com/1424-8247/9/2/27adrenoblockersα-adrenoblockersheterocyclesthiadiazines1,3,4-thiadiazine-2-aminesserotoninstresspharmacological evaluation |
| spellingShingle | Alexey P. Sarapultsev Oleg N. Chupakhin Petr A. Sarapultsev Larisa P. Sidorova Tatiana A. Tseitler Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide Pharmaceuticals adrenoblockers α-adrenoblockers heterocycles thiadiazines 1,3,4-thiadiazine-2-amines serotonin stress pharmacological evaluation |
| title | Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide |
| title_full | Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide |
| title_fullStr | Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide |
| title_full_unstemmed | Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide |
| title_short | Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide |
| title_sort | pharmacologic evaluation of antidepressant activity and synthesis of 2 morpholino 5 phenyl 6h 1 3 4 thiadiazine hydrobromide |
| topic | adrenoblockers α-adrenoblockers heterocycles thiadiazines 1,3,4-thiadiazine-2-amines serotonin stress pharmacological evaluation |
| url | http://www.mdpi.com/1424-8247/9/2/27 |
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