Title of article :
Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity
Author/Authors :
Kenneth M. Boy، نويسنده , , Michael Dee، نويسنده , , Joseph Yevich، نويسنده , , John Torrente، نويسنده , , Qi Gao، نويسنده , , Lawrence Iben، نويسنده , , Arlene Stark، نويسنده , , Ronald J. Mattson، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2004
Abstract :
Conformationally constrained aryl cyclohexanes and cyclohexenes based on aryl cyclohexanols 1 were prepared. Locking the aryl ring in plane with the cyclohexane moiety provided potent SSRIs 3. Conversely, fixing the aryl ring perpendicular to the cyclohexane ring via a spiro lactone provided balanced 5-HT1A antagonists with mid-nanomolar range SSRI potency (compounds 2).
Keywords :
erotonin , SSRI , 5-HT1a , Depression.* Corresponding author. Tel.: +1-203-677-6278 , fax: +1-203-677-7702 , e-mail: boyk@bms.com
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
