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  • Title: Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.
    Author: Takeuchi K, Kohn TJ, Honigschmidt NA, Rocco VP, Spinazze PG, Koch DJ, Nelson DL, Wainscott DB, Ahmad LJ, Shaw J, Threlkeld PG, Wong DT.
    Journal: Bioorg Med Chem Lett; 2003 Jun 02; 13(11):1903-5. PubMed ID: 12749894.
    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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