Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors |
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| Authors: | Shao Liming Wang Fengjiang Malcolm Scott C Ma Jianguo Hewitt Michael C Campbell Una C Bush Larry R Spicer Nancy A Engel Sharon R Saraswat Lakshmi D Hardy Larry W Koch Patrick Schreiber Rudy Spear Kerry L Varney Mark A |
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| Affiliation: | Discovery and Early Clinical Research, Sepracor Inc., 84 Waterford Drive, Marlborough, MA 01752, USA |
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| Abstract: | The present work describes a series of novel chiral amines that potently inhibit the in vitro reuptake of serotonin, norepinephrine and dopamine (triple reuptake inhibitors) and were active in vivo in a mouse model predictive of antidepressant like activity. The detailed synthesis and in vitro activity and ADME profile of compounds is described, which represent a previously undisclosed triple reuptake inhibitor chemotype. |
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| Keywords: | Triple uptake inhibitor (TRI) Depression Antidepressant Monoamine transporter |
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