title: Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 4.
abstract: 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.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA.
authors.forename: Vincent P
authors.initials: VP
authors.lastname: Rocco
authors.forename: Patrick G
authors.initials: PG
authors.lastname: Spinazze
authors.forename: Todd J
authors.initials: TJ
authors.lastname: Kohn
authors.forename: Nicholas A
authors.initials: NA
authors.lastname: Honigschmidt
authors.forename: David L
authors.initials: DL
authors.lastname: Nelson
authors.forename: D
authors.initials: D
authors.lastname: Bradley Wainscott
authors.forename: Laura J
authors.initials: LJ
authors.lastname: Ahmad
authors.forename: Janice
authors.initials: J
authors.lastname: Shaw
authors.forename: Penny G
authors.initials: PG
authors.lastname: Threlkeld
authors.forename: David T
authors.initials: DT
authors.lastname: Wong
authors.forename: Kumiko
authors.initials: K
authors.lastname: Takeuchi
mesh_terms: 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
chemical_list: 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