Novel aryloxy-8-azabicyclo[3.2.1]oct-3-enes with 5-HT transporter and 5-HT1A affinity |
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| Authors: | Gilbert Adam M Coleman Thomas Kodah Jason Mewshaw Richard E Scerni Rosemary Schechter Lee E Smith Deborah L Andree Terrance H |
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| Institution: | Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965-1215, USA. gilbera@wyeth.com |
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| Abstract: | Joining aryl 8-azabicyclo3.2.1]oct-3-enes with aryloxyethanes and aryloxypropanes produces novel series of compounds 11 and 12 with potent 5-HT-T affinity and moderately potent 5-HT(1A) affinity. Moreover, several of these compounds possess functional 5-HT(1A) antagonism. Optimal compounds are, 4-indolyloxyethane 21, 4-indolyloxypropanes 25, and 27, which possess potent 5-HT-T affinity (5-HT-T K(i): 21: 1.2nM, 25: 0.54nM, 27: 0.38nM) and good 5-HT(1A) affinity/antagonism (5-HT(1A)K(i), (35)S]GTPgammaS: E(max) (%): 21: 111.1nM, 0%; 25: 173.2nM, 0%; 27: 107nM, 0%). |
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