Discovery of a new series of 5-HT1A receptor agonists |
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| Authors: | Silvia Franchini Adolfo Prandi Claudia Sorbi Annalisa Tait Annamaria Baraldi Piero Angeli Michela Buccioni Antonio Cilia Elena Poggesi Paola Fossa Livio Brasili |
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| Affiliation: | 1. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Modena e Reggio Emilia, Via Campi 183, 41100 Modena, Italy;2. Dipartimento di Scienze Chimiche, Università degli Studi di Camerino, Via S. Agostino 1, 62032 Camerino, Italy;3. Divisione Ricerca e Sviluppo, Recordati S.p.A., Via Civitali 1, 20148 Milano, Italy;4. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Genova, Viale Benedetto XV 3, 16132 Genova, Italy |
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| Abstract: | Starting from compounds previously identified as α1-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/α1 = 151) and good agonist potency (pD2 = 7.82; Emax = 76), was found to be the most interesting. |
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