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Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2011-01-12 , DOI: 10.1016/j.bmcl.2011.01.016 Liming Shao , Michael C. Hewitt , Fengjiang Wang , Scott C. Malcolm , Jianguo Ma , John E. Campbell , Una C. Campbell , Sharon R. Engel , Nancy A. Spicer , Larry W. Hardy , Rudy Schreiber , Kerry L. Spear , Mark A. Varney
中文翻译:
的发现ñ -甲基-1-(1-苯基环己基)甲胺,一种新型的三羟色胺,去甲肾上腺素和多巴胺再摄取抑制剂
更新日期:2011-01-12
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2011-01-12 , DOI: 10.1016/j.bmcl.2011.01.016 Liming Shao , Michael C. Hewitt , Fengjiang Wang , Scott C. Malcolm , Jianguo Ma , John E. Campbell , Una C. Campbell , Sharon R. Engel , Nancy A. Spicer , Larry W. Hardy , Rudy Schreiber , Kerry L. Spear , Mark A. Varney
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, IC50 = 169, 85, 21 nM) and 42 (SERT, NET, DAT IC50 = 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.
中文翻译:
的发现ñ -甲基-1-(1-苯基环己基)甲胺,一种新型的三羟色胺,去甲肾上腺素和多巴胺再摄取抑制剂
当前的工作公开了一种新型的环己基芳基胺化学型,其具有对5-羟色胺,去甲肾上腺素和多巴胺转运蛋白的有效抑制作用,并且具有治疗重度抑郁症的潜力。优化的化合物1(SERT,NET,DAT,IC 50 = 169,85,21 nM)和42(SERT,NET,DAT IC 50 = 34,295,90 nM)具有高脑渗透性,在小鼠尾巴中具有体内活性悬架试验在30 mpk po时进行,不是一般的运动兴奋剂。