Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4.
A series of 1-(1H-indol-4-yloxy)-3-(4-arylpiperidinyl)propan-2-ols possessing potent dual 5-HT(1A) receptor antagonism and serotonin reuptake inhibition was discovered. The fused aryl ring moiety contributed to the robust dual activities irrespective of the regiochemistry associated with its connectivity to the piperidine central ring.
Rocco
Vincent P
VP
Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA.
Spinazze
Patrick G
PG
Kohn
Todd J
TJ
Honigschmidt
Nicholas A
NA
Nelson
David L
DL
Bradley Wainscott
D
D
Ahmad
Laura J
LJ
Shaw
Janice
J
Threlkeld
Penny G
PG
Wong
David T
DT
Takeuchi
Kumiko
K
D018687:Antidepressive Agents, Second-Generation / Q000138:chemical synthesis* / Q000494:pharmacology; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000494:pharmacology; D020005:Propanols / Q000138:chemical synthesis / Q000494:pharmacology*; D011485:Protein Binding; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D018687:Antidepressive Agents, Second-Generation; D006576:Heterocyclic Compounds, 4 or More Rings; D020005:Propanols; D058829:Serotonin 5-HT1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors