Novel 5-HT1A/1B/1D receptors antagonists with potent 5-HT reuptake inhibitory activity

Abstract Novel 2-methyl-5-quinolinyl-1-piperazinylalkyl-3,4-dihydro-2 H -1,4-benzoxazin-3-ones showing high affinities for the 5-HT 1A/1B/1D receptors coupled with potent 5-HT reuptake inhibitory activity have been discovered. This is the first report describing docking of the lead compound 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2 H -1,4-benzoxazin-3(4 H )-one 1 , into a model of the 5-HT transporter and the 5-HT 1A receptor model.