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Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, 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. 1434-7. Date of Electronic Publication: 2011 Jan 12. - Publication Year :
- 2011
-
Abstract
- Novel chiral cyclohexylaryl amines were developed with potent reuptake inhibition against the serotonin, norepinephrine and dopamine transporters and activity at 10 and 30 mpk PO in the mouse tail suspension test. Prototype compound 31 (SERT, NET, DAT IC(50) ≤ 1, 21, 28 nM) was highly brain penetrant, had minimal CYP and hERG inhibition, and represents a previously undisclosed architecture with potential for treatment of major depressive disorder.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amines chemistry
Amines pharmacology
Animals
Cyclization
Inhibitory Concentration 50
Mice
Molecular Structure
Stereoisomerism
Amines chemical synthesis
Dopamine Uptake Inhibitors chemical synthesis
Dopamine Uptake Inhibitors chemistry
Dopamine Uptake Inhibitors pharmacology
Drug Design
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 :
- 21310612
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.01.019