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Shao, Liming; Hewitt, Michael C.; Wang, Fengjiang; Malcolm, Scott C.; Ma, Jianguo; Campbell, John E.; Campbell, Una C.; Engel, Sharon R.; Spicer, Nancy A.; Hardy, Larry W.; Schreiber, Rudy; Spear, Kerry L.; Varney, Mark A.
Bioorganic & medicinal chemistry letters, 03/2011, Letnik: 21, Številka: 5Journal Article
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.
