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Elsevier, Bioorganic and Medicinal Chemistry Letters, 6(20), p. 2017-2020

DOI: 10.1016/j.bmcl.2010.01.030

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Discovery of a new series of 5-HT1A receptor agonists

Journal article published in 2010 by Silvia Franchini ORCID, Adolfo Prandi, Claudia Sorbi, Annalisa Tait ORCID, Annamaria Baraldi, Piero Angeli, Michela Buccioni, Antonio Cilia, Elena Poggesi, Paola Fossa, Livio Brasili ORCID
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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Abstract

Starting from compounds previously identified as alpha(1)-adrenoceptor antagonists that were also found to bind to the 5-HT(1A) receptor, in an attempt to separate the two activities, a new series of 5-HT(1A) receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity (5-HT(1A)/alpha(1)=151) and good agonist potency (pD(2)=7.82; E(max)=76), was found to be the most interesting.