Design and Synthesis of Arylamidine Derivatives as Serotonin/Norepinephrine Dual Reuptake Inhibitors
| Autor: | Wen Qin, Hui Wen, Yan-shen Guo, Guangzhong Yang |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Magnetic Resonance Spectroscopy
Pharmaceutical Science Chemistry Techniques Synthetic Pharmacology 01 natural sciences Article norepinephrine Analytical Chemistry Reuptake lcsh:QD241-441 Norepinephrine (medication) Inhibitory Concentration 50 Structure-Activity Relationship dual reuptake inhibitors lcsh:Organic chemistry In vivo Drug Discovery medicine Animals Physical and Theoretical Chemistry IC50 antidepressant Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Antidepressive Agents Acute toxicity Rats serotonin 0104 chemical sciences 010404 medicinal & biomolecular chemistry Chemistry (miscellaneous) Drug Design Molecular Medicine Antidepressant Serotonin Reuptake inhibitor Selective Serotonin Reuptake Inhibitors medicine.drug |
| Zdroj: | Molecules Volume 24 Issue 3 Molecules, Vol 24, Iss 3, p 497 (2019) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules24030497 |
| Popis: | To improve the in vivo antidepressant activity of previously reported serotonin (5-HT) and norepinephrine (NE) dual reuptake inhibitors, three series of arylamidine derivatives were designed and synthesized. The in vitro 5-HT and NE reuptake inhibitory activities of these compounds were evaluated, and compound II-5 was identified as the most potent 5-HT (IC50 = 620 nM) and NE (IC50 = 10 nM) dual reuptake inhibitor. Compound II-5 exhibited potent antidepressant activity in the rat tail suspension test and showed an acceptable safety profile in a preliminary acute toxicity test in mice. Our results show that these arylamidine derivatives exhibit potent 5-HT/NE dual reuptake inhibition and should be explored further as antidepressant drug candidates. |
| Databáze: | OpenAIRE |
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