| Literature DB >> 15664848 |
Peter J Atkinson1, Steven M Bromidge, Mark S Duxon, Laramie M Gaster, Michael S Hadley, Beverley Hammond, Christopher N Johnson, Derek N Middlemiss, Stephanie E North, Gary W 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 K K Vong, Jeannette M Watson.
Abstract
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-HT(1A) receptor and potent 5-HT reuptake inhibitory activity. The 5-(2-methyl)quinolinyloxy derivative combined high 5-HT(1A/1B/1D) receptor affinities with low intrinsic activity and potent inhibition of the 5-HT reuptake site (pK(i)8.2). This compound also had good oral bioavailability and brain penetration in the rat.Entities:
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Year: 2005 PMID： 15664848 DOI： 10.1016/j.bmcl.2004.11.030
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823