Literature DB >> 18829312

Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.

Halina T Serafinowska1, Frank E Blaney, Peter J Lovell, Giancarlo G Merlo, Claire M Scott, Paul W Smith, Kathryn R Starr, Jeannette M Watson.   

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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Year:  2008        PMID: 18829312     DOI: 10.1016/j.bmcl.2008.08.110

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  5-HT1A receptor pharmacophores to screen for off-target activity of α1-adrenoceptor antagonists.

Authors:  Tony Ngo; Timothy J Nicholas; Junli Chen; Angela M Finch; Renate Griffith
Journal:  J Comput Aided Mol Des       Date:  2013-04-27       Impact factor: 3.686

2.  Palladium-catalyzed amination of dichloroquinolines with adamantane-containing amines.

Authors:  Anton S Abel; Alexei D Averin; Olga A Maloshitskaya; Evgenii N Savelyev; Boris S Orlinson; Ivan A Novakov; Irina P Beletskaya
Journal:  Molecules       Date:  2013-02-06       Impact factor: 4.411

  2 in total

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