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BIBTEX RIS

3,4-Dihydro-2H-benzoxazinones are 5-HT1A receptor antagonists with potent 5-HT reuptake inhibitory activity

2004; Elsevier BV; Volume: 15; Issue: 3 Linguagem: Inglês

10.1016/j.bmcl.2004.11.030

ISSN

1464-3405

Autores

Peter J. Atkinson, Steven M. Bromidge, Mark Duxon, Laramie M. Gaster, Michael S. Hadley, Beverley Hammond, Christopher N. Johnson, Derek N. Middlemiss, Stephanie E. North, Gary Price, Harshad K. Rami, Graham J. Riley, Claire M. Scott, Tracey E. Shaw, Kathryn R. Starr, Geoffrey Stemp, Kevin M. Thewlis, David R. Thomas, Mervyn Thompson, Antonio Vong, Jeannette M. Watson,

Tópico(s)

Neurotransmitter Receptor Influence on Behavior

Resumo

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 (pKi 8.2). This compound also had good oral bioavailability and brain penetration in the rat.

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