Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity |
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| Authors: | Boy Kenneth M Dee Michael Yevich Joseph Torrente John Gao Qi Iben Lawrence Stark Arlene Mattson Ronald J |
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| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. boyk@bms.com |
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| 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). |
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