Amphetamine Derivatives as Potent Central Nervous System Multitarget SERT/NET/H 3 Agents: Synthesis and Biological Evaluation.
| Title: | Amphetamine Derivatives as Potent Central Nervous System Multitarget SERT/NET/H 3 Agents: Synthesis and Biological Evaluation. |
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| Authors: | Li, Quxiang, Ren, Lili, Wang, Dongli, Luo, Junyong, Xu, Changda, Feng, Jian, Qiu, Yufan, Xu, Xiangqing, Chen, Guoguang |
| Source: | Molecules; Nov2024, Vol. 29 Issue 22, p5240, 19p |
| Subject Terms: | HISTAMINE receptors, BIOSYNTHESIS, SEROTONIN transporters, MOLECULAR docking, CENTRAL nervous system, H2 receptor antagonists, ANTIDEPRESSANTS |
| Abstract: | In this research, a variety of novel amphetamine derivatives were synthesized and assessed for their potential as multifaceted antidepressant agents. Among these compounds, compound 11b demonstrated potent inhibitory effects on both serotonin and noradrenaline transporters (SERT/NET) and high affinity for histamine H |
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| Database: | Complementary Index |
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| Header | DbId: edb DbLabel: Complementary Index An: 181202894 RelevancyScore: 1060 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 1060.21044921875 |
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| Items | – Name: Title Label: Title Group: Ti Data: Amphetamine Derivatives as Potent Central Nervous System Multitarget SERT/NET/H 3 Agents: Synthesis and Biological Evaluation. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Li%2C+Quxiang%22">Li, Quxiang</searchLink><br /><searchLink fieldCode="AR" term="%22Ren%2C+Lili%22">Ren, Lili</searchLink><br /><searchLink fieldCode="AR" term="%22Wang%2C+Dongli%22">Wang, Dongli</searchLink><br /><searchLink fieldCode="AR" term="%22Luo%2C+Junyong%22">Luo, Junyong</searchLink><br /><searchLink fieldCode="AR" term="%22Xu%2C+Changda%22">Xu, Changda</searchLink><br /><searchLink fieldCode="AR" term="%22Feng%2C+Jian%22">Feng, Jian</searchLink><br /><searchLink fieldCode="AR" term="%22Qiu%2C+Yufan%22">Qiu, Yufan</searchLink><br /><searchLink fieldCode="AR" term="%22Xu%2C+Xiangqing%22">Xu, Xiangqing</searchLink><br /><searchLink fieldCode="AR" term="%22Chen%2C+Guoguang%22">Chen, Guoguang</searchLink> – Name: TitleSource Label: Source Group: Src Data: Molecules; Nov2024, Vol. 29 Issue 22, p5240, 19p – Name: Subject Label: Subject Terms Group: Su Data: <searchLink fieldCode="DE" term="%22HISTAMINE+receptors%22">HISTAMINE receptors</searchLink><br /><searchLink fieldCode="DE" term="%22BIOSYNTHESIS%22">BIOSYNTHESIS</searchLink><br /><searchLink fieldCode="DE" term="%22SEROTONIN+transporters%22">SEROTONIN transporters</searchLink><br /><searchLink fieldCode="DE" term="%22MOLECULAR+docking%22">MOLECULAR docking</searchLink><br /><searchLink fieldCode="DE" term="%22CENTRAL+nervous+system%22">CENTRAL nervous system</searchLink><br /><searchLink fieldCode="DE" term="%22H2+receptor+antagonists%22">H2 receptor antagonists</searchLink><br /><searchLink fieldCode="DE" term="%22ANTIDEPRESSANTS%22">ANTIDEPRESSANTS</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: In this research, a variety of novel amphetamine derivatives were synthesized and assessed for their potential as multifaceted antidepressant agents. Among these compounds, compound 11b demonstrated potent inhibitory effects on both serotonin and noradrenaline transporters (SERT/NET) and high affinity for histamine H<subscript>3</subscript> receptor (H<subscript>3</subscript>R), and displayed low affinity for off-target receptors (H1, α1) and hERG channels, which can reduce the prolongation of the QT interval. Molecular docking studies offered a rational binding model of compound 11b when it forms a complex with SERT, NET, and the histamine H<subscript>3</subscript> receptor. In vivo behavioral studies, compound 11b dose-dependently reduced the immobility duration in the mouse FST and TST assays without a stimulatory effect on the locomotor activity. Furthermore, compound 11b had a favorable pharmacokinetic profile in rats. Thus, compound 11b has the potential to develop a novel class of drugs for the treatment of depression. [ABSTRACT FROM AUTHOR] – Name: Abstract Label: Group: Ab Data: <i>Copyright of Molecules is the property of MDPI and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.3390/molecules29225240 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 19 StartPage: 5240 Subjects: – SubjectFull: HISTAMINE receptors Type: general – SubjectFull: BIOSYNTHESIS Type: general – SubjectFull: SEROTONIN transporters Type: general – SubjectFull: MOLECULAR docking Type: general – SubjectFull: CENTRAL nervous system Type: general – SubjectFull: H2 receptor antagonists Type: general – SubjectFull: ANTIDEPRESSANTS Type: general Titles: – TitleFull: Amphetamine Derivatives as Potent Central Nervous System Multitarget SERT/NET/H 3 Agents: Synthesis and Biological Evaluation. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Li, Quxiang – PersonEntity: Name: NameFull: Ren, Lili – PersonEntity: Name: NameFull: Wang, Dongli – PersonEntity: Name: NameFull: Luo, Junyong – PersonEntity: Name: NameFull: Xu, Changda – PersonEntity: Name: NameFull: Feng, Jian – PersonEntity: Name: NameFull: Qiu, Yufan – PersonEntity: Name: NameFull: Xu, Xiangqing – PersonEntity: Name: NameFull: Chen, Guoguang IsPartOfRelationships: – BibEntity: Dates: – D: 15 M: 11 Text: Nov2024 Type: published Y: 2024 Identifiers: – Type: issn-print Value: 14203049 Numbering: – Type: volume Value: 29 – Type: issue Value: 22 Titles: – TitleFull: Molecules Type: main |
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