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Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 01; Vol. 21 (1), pp. 520-3. Date of Electronic Publication: 2010 Oct 28. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Dopamine Plasma Membrane Transport Proteins metabolism
Dopamine Uptake Inhibitors chemical synthesis
Dopamine Uptake Inhibitors pharmacokinetics
Drug Evaluation, Preclinical
Humans
Mice
Microsomes metabolism
Quinolines chemical synthesis
Quinolines pharmacokinetics
Serotonin Plasma Membrane Transport Proteins metabolism
Selective Serotonin Reuptake Inhibitors chemical synthesis
Selective Serotonin Reuptake Inhibitors pharmacokinetics
Dopamine Plasma Membrane Transport Proteins antagonists & inhibitors
Dopamine Uptake Inhibitors chemistry
Quinolines chemistry
Serotonin Plasma Membrane Transport Proteins chemistry
Selective Serotonin Reuptake Inhibitors chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21095126
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.086