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Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Mar 01; Vol. 21 (5), pp. 1438-41. Date of Electronic Publication: 2011 Jan 12. - Publication Year :
- 2011
-
Abstract
- The current work discloses a novel cyclohexylarylamine chemotype with potent inhibition of the serotonin, norepinephrine, and dopamine transporters and potential for treatment of major depressive disorder. Optimized compounds 1 (SERT, NET, DAT, IC(50)=169, 85, 21 nM) and 42 (SERT, NET, DAT IC(50)=34, 295, 90 nM) were highly brain penetrant, active in vivo in the mouse tail suspension test at 30 mpk po and were not general motor stimulants.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amines chemistry
Amines pharmacology
Animals
Antidepressive Agents chemical synthesis
Antidepressive Agents chemistry
Antidepressive Agents pharmacology
Cyclization
Inhibitory Concentration 50
Methane chemistry
Methane pharmacology
Mice
Molecular Structure
Rats
Stereoisomerism
Amines chemical synthesis
Dopamine Uptake Inhibitors chemical synthesis
Dopamine Uptake Inhibitors chemistry
Dopamine Uptake Inhibitors pharmacology
Drug Design
Methane chemical synthesis
Norepinephrine chemical synthesis
Norepinephrine chemistry
Norepinephrine pharmacology
Serotonin chemical synthesis
Serotonin chemistry
Serotonin pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21310609
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.01.016