title: Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.
abstract: Analogues of pindolol, 1-(1H-indol-4-yloxy)-3-isopropylamino-propan-2-ol, were synthesized and evaluated as 5-HT(1A) receptor antagonists. The structural features required for optimal binding to the 5-HT1A receptor are as follows: S-2-propanol linker, 4-indoloxy substituent, and a large lipophilic cyclic amine substituent.
authors.affiliation: Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA. krush@lilly.com
authors.forename: Joseph H
authors.initials: JH
authors.lastname: Krushinski
authors.forename: John M
authors.initials: JM
authors.lastname: Schaus
authors.forename: Dennis C
authors.initials: DC
authors.lastname: Thompson
authors.forename: David O
authors.initials: DO
authors.lastname: Calligaro
authors.forename: David L
authors.initials: DL
authors.lastname: Nelson
authors.forename: Susan H
authors.initials: SH
authors.lastname: Luecke
authors.forename: David B
authors.initials: DB
authors.lastname: Wainscott
authors.forename: David T
authors.initials: DT
authors.lastname: Wong
mesh_terms: D000818:Animals; D003345:Corticosterone / Q000097:blood; D006900:Hydroxylation; D007211:Indoles / Q000737:chemistry*; D007536:Isomerism; D008297:Male; D015394:Molecular Structure; D010084:Oxidation-Reduction; D011412:Propanolamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D058829:Serotonin 5-HT1 Receptor Antagonists; D013329:Structure-Activity Relationship