Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 3.
A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT(1A) 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.
Takeuchi
Kumiko
K
Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA. ktak@lilly.com
Kohn
Todd J
TJ
Honigschmidt
Nicholas A
NA
Rocco
Vincent P
VP
Spinazze
Patrick G
PG
Atkinson
Steven T
ST
Hertel
Larry W
LW
Nelson
David L
DL
Wainscott
D Bradley
DB
Ahmad
Laura J
LJ
Shaw
Janice
J
Threlkeld
Penny G
PG
Wong
David T
DT
D000928:Antidepressive Agents / Q000138:chemical synthesis*; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D007202:Indicators and Reagents; D008968:Molecular Conformation; D015394:Molecular Structure; D017374:Paroxetine / Q000494:pharmacology; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D020005:Propanols / Q000138:chemical synthesis* / Q000494:pharmacology; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D007202:Indicators and Reagents; D017374:Paroxetine; D010880:Piperidines; D020005:Propanols; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors