3, 4-Dihydro-2H-benzoxazinones are 5-HT 1A receptor antagonists with potent 5-HT reuptake inhibitory activity

…, B Hammond, CN Johnson, DN Middlemiss…

文献索引：Atkinson, Peter J.; Bromidge, Steven M.; Duxon, Mark S.; Gaster, Laramie M.; Hadley, Michael S.; Hammond, Beverley; Johnson, Christopher N.; Middlemiss, Derek N.; North, Stephanie E.; Price, Gary W.; Rami, Harshad K.; Riley, Graham J.; Scott, Claire M.; Shaw, Tracey E.; Starr, Kathryn R.; Stemp, Geoffrey; Thewlis, Kevin M.; Thomas, David R.; Thompson, Mervyn; Vong, Antonio K.K.; Watson, Jeannette M. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 737 - 741

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被引用次数: 56

摘要

Starting from a high throughput screening hit, a series of 3, 4-dihydro-2H-benzoxazinones has been identified with both high affinity for the 5-HT1A receptor and potent 5-HT reuptake inhibitory activity. The 5-(2-methyl) quinolinyloxy derivative combined high 5-HT1A/1B/1D receptor affinities with low intrinsic activity and potent inhibition of the 5-HT reuptake site (pKi8. 2). This compound also had good oral bioavailability and brain penetration in the ...