Title of article
Advances toward new antidepressants beyond SSRIs: 1-Aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5
Author/Authors
Kumiko Takeuchi، نويسنده , , Todd J. Kohn، نويسنده , , Nicholas A. Honigschmidt، نويسنده , , Vincent P. Rocco، نويسنده , , Patrick G. Spinazze، نويسنده , , Susan K. Hemrick-Luecke، نويسنده , , Linda K. Thompson، نويسنده , , David C. Evans، نويسنده , , Kurt Rasmussen، نويسنده , , Deanna Koger، نويسنده , , David Lodge، نويسنده , , Laura J. Martin، نويسنده , , Janice Shaw، نويسنده , , Penny G. Threlkeld، نويسنده , , David T. Wong، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
2347
To page
2351
Abstract
A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A 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 affinities at the 5-HT1A receptor and serotonin reuptake site in vitro. In vivo evaluation of this series of compounds demonstrated elevated extracellular serotonin levels from the basal and quick recovery of neuron firing that was presumably suppressed by the initial acute activation of 5-HT1A somatodendritic autoreceptors.
Keywords
Serotonin , 5- HT1A receptor antagonist , Selective serotonin reuptake inhibitor , 5-HT1A/SSRI , Antidepressants , 1-Aryloxy-3-piperidinylpropan-2-ols
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796778
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