Abstract
Starting from a high throughput screening hit, a series of 3,4-dihydro-2 H-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 (p K i 8.2). This compound also had good oral bioavailability and brain penetration in the rat.
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