Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 1.
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.
Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA. ktak@lilly.com
Kumiko
K
Takeuchi
Todd J
TJ
Kohn
Nicholas A
NA
Honigschmidt
Vincent P
VP
Rocco
Patrick G
PG
Spinazze
Daniel J
DJ
Koch
David L
DL
Nelson
D Bradley
DB
Wainscott
Laura J
LJ
Ahmad
Janice
J
Shaw
Penny G
PG
Threlkeld
David T
DT
Wong
D018687:Antidepressive Agents, Second-Generation / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D017374:Paroxetine / Q000494:pharmacology; D020005:Propanols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D018687:Antidepressive Agents, Second-Generation; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D007211:Indoles; D017374:Paroxetine; D020005:Propanols; D044282:Receptor, Serotonin, 5-HT1A; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors