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Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists. 2007
Joseph H Krushinski, and
John M Schaus, and
Dennis C Thompson, and
David O Calligaro, and
David L Nelson, and
Susan H Luecke, and
David B Wainscott, and
David T Wong
Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA. krush@lilly.com
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.
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