Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 6, Pages 2017-2020Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.030
Keywords
5-HT1A receptor; Agonists; 1,3-Dioxolane; Selectivity
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Funding
- Italian Ministry for University and Research
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Starting from compounds previously identified as alpha(1)-adrenoceptor antagonists that were also found to bind to the 5-HT1A receptor, in an attempt to separate the two activities, a new series of 5-HT1A receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT1A/alpha(1) = 151) and good agonist potency (pD(2) = 7.82; E-max = 76), was found to be the most interesting. (C) 2010 Elsevier Ltd. All rights reserved.
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