Starting from compounds previously disclosed as 1-adrenoceptor antagonists which were also found to bind to 5-HT1A receptor, in the attempt to separate the two activities, a new series of 5-HT1A receptor agonist was identified. They were shown to have high potency and/or high selectivity. Among them compound 13 that combine high selectivity (5-HT1A/1= 151) and good agonist potency (pD2= 7.82; Emax=76) turned out to be the most interesting of the series.
Discovery of a new series of 5-HT1A receptor agonists / Franchini, Silvia; Prandi, Adolfo; Sorbi, Claudia; Tait, Annalisa; Annamaria, Baraldi; Piero, Angeli; Michela, Buccioni; Antonio, Cilia; Elena, Poggesi; Paola, Fossa; Brasili, Livio. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 20:(2010), pp. 2017-2020. [10.1016/j.bmcl.2010.01.030]
Discovery of a new series of 5-HT1A receptor agonists
FRANCHINI, Silvia;PRANDI, adolfo;SORBI, Claudia;TAIT, Annalisa;BRASILI, Livio
2010
Abstract
Starting from compounds previously disclosed as 1-adrenoceptor antagonists which were also found to bind to 5-HT1A receptor, in the attempt to separate the two activities, a new series of 5-HT1A receptor agonist was identified. They were shown to have high potency and/or high selectivity. Among them compound 13 that combine high selectivity (5-HT1A/1= 151) and good agonist potency (pD2= 7.82; Emax=76) turned out to be the most interesting of the series.
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