Starting from compound 1, a previously reported a1D-adrenoceptorsantagonist, a new series of ligands acting at 5-HT1A serotoninreceptor were identified through simple structure modifications.Among them (2,2-diphenyl-[1,3]oxathiolan-5-yl-methyl)-(3-phenylpropyl)amine (19) exhibits outstanding activity (pKi=8.72, pD2=7.67, Emax=85) and selectivity (5-HT1A/a1D>150), and representsan as yet unidentified 5-HT1A agonist scaffold.
(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenylpropyl)-amine: a Potent and Selective 5-HT1A Receptor Agonist / Franchini, Silvia; Tait, Annalisa; Prandi, Adolfo; Sorbi, Claudia; Gallesi, Rossella; M., Buccioni; G., Marucci; C., De Stefani; A., Cilia; Brasili, Livio. - In: CHEMMEDCHEM. - ISSN 1860-7179. - STAMPA. - 4:2(2009), pp. 196-203. [10.1002/cmdc.200800276]
(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenylpropyl)-amine: a Potent and Selective 5-HT1A Receptor Agonist
FRANCHINI, Silvia;TAIT, Annalisa;PRANDI, adolfo;SORBI, Claudia;GALLESI, Rossella;BRASILI, Livio
2009
Abstract
Starting from compound 1, a previously reported a1D-adrenoceptorsantagonist, a new series of ligands acting at 5-HT1A serotoninreceptor were identified through simple structure modifications.Among them (2,2-diphenyl-[1,3]oxathiolan-5-yl-methyl)-(3-phenylpropyl)amine (19) exhibits outstanding activity (pKi=8.72, pD2=7.67, Emax=85) and selectivity (5-HT1A/a1D>150), and representsan as yet unidentified 5-HT1A agonist scaffold.
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