Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor
Active in mouse tail suspension test at 10 and 30 mpk PO. 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,...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-03, Vol.21 (5), p.1434-1437 |
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Hauptverfasser: | , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
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Zusammenfassung: | Active in mouse tail suspension test at 10 and 30
mpk PO.
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2011.01.019 |