Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor |
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Authors: | Shao Liming Ma Jianguo Wang Fengjiang Malcolm Scott C Hewitt Michael C Campbell Una C Spicer Nancy A Hardy Larry W Schreiber Rudy Spear Kerry L Varney Mark A |
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Institution: | Discovery and Early Clinical Research, Sunovion Pharmaceuticals Inc, 84 Waterford Drive, Marlborough, MA 01752, USA. liming.shao@sunovion.com |
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Abstract: | The present work describes a series of novel tetrahydroquinoline amines that potently inhibit the in vitro reuptake of serotonin and dopamine (dual reuptake inhibitors). The compounds are structurally related to a series we disclosed previously, but are improved with respect to cytochrome P-450 enzyme (CYP) and potassium ion channel Kv11.1 (hERG) inhibition and synthetic accessibility. The detailed synthesis and in vitro activity and ADME profile of the compounds is described, which represent a previously undisclosed dual reuptake inhibitor chemotype. |
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