1.Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor.
Shao L1, Hewitt MC, Wang F, Malcolm SC, Ma J, Campbell JE, Campbell UC, Engel SR, Spicer NA, Hardy LW, Schreiber R, Spear KL, Varney MA. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1438-41. doi: 10.1016/j.bmcl.2011.01.016. Epub 2011 Jan 12.
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.