Literature DB >> 12749894

Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.

Kumiko Takeuchi1, Todd J Kohn, Nicholas A Honigschmidt, Vincent P Rocco, Patrick G Spinazze, Daniel J Koch, David L Nelson, D Bradley Wainscott, Laura J Ahmad, Janice Shaw, Penny G Threlkeld, David T Wong.   

Abstract

A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT(1A) receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinity at the 5-HT(1A) receptor and serotonin reuptake inhibition at nanomolar concentrations for dual activities.

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Year:  2003        PMID： 12749894     DOI： 10.1016/s0960-894x(03)00303-2

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


  2 in total

1.  Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands.

Authors:  Xiaobo Gu; Sari Izenwasser; Dean Wade; Amy Housman; Gerard Gulasey; Jill B Rhoden; Christopher D Savoie; David L Mobley; Stacey A Lomenzo; Mark L Trudell
Journal:  Bioorg Med Chem       Date:  2010-09-29       Impact factor: 3.641

2.  Antidepressant potential of nitrogen-containing heterocyclic moieties: An updated review.

Authors:  Nadeem Siddiqui; Sandhya Bawa; Ruhi Ali; Obaid Afzal; M Jawaid Akhtar; Bishmillah Azad; Rajiv Kumar
Journal:  J Pharm Bioallied Sci       Date:  2011-04
  2 in total

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