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

Kumiko Takeuchi,Todd J Kohn,Nicholas A Honigschmidt,Vincent P Rocco,Patrick G Spinazze,Steven T Atkinson,Larry W Hertel,David L Nelson,D.Bradley Wainscott,Laura J Ahmad,Janice Shaw,Penny G Threlkeld,David T Wong

Bioorganic & Medicinal Chemistry Letters（2003）

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摘要

A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered. Modification of potential metabolic sites of 1-(1H-indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols further improved the in vitro binding affinities and functional antagonism.

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