Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity |
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| Authors: | Serafinowska Halina T Blaney Frank E Lovell Peter J Merlo Giancarlo G Scott Claire M Smith Paul W Starr Kathryn R Watson Jeannette M |
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| Institution: | Neurosciences CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. halina.serafinowska@gsk.com |
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| Abstract: | Novel 2-methyl-5-quinolinyl-1-piperazinylalkyl-3,4-dihydro-2H-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}-2H-1,4-benzoxazin-3(4H)-one 1, into a model of the 5-HT transporter and the 5-HT(1A) receptor model. |
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