(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenyl-propyl)-amine: a Potent and Selective 5-HT1A Receptor Agonist

Franchini, S.; Tait, A.; Prandi, A.; Sorbi, C.; Gallesi, R.; Buccioni, Michela; Marucci, Gabriella; De Stefani, C.; Cilia, A.; Brasili, L.

Starting from compound 1, a previously reported a1D-adrenocep- tors antagonist, a new series of ligands acting at 5-HT1A serotonin receptor were identified through simple structure modifications. Among them (2,2-diphenyl-[1,3]oxathiolan-5-yl-methyl)-(3-phenylpropylamine (19) exhibits outstanding activity (pKi=8.72, pD2=7.67, E max=85) and selectivity (5-HT1A/α1D, 150), and represents an as yet unidentified 5-HT1A agonist scaffold.

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Titolo:	(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenyl-propyl)-amine: a Potent and Selective 5-HT1A Receptor Agonist
Autori:	FRANCHINI S. TAIT A. PRANDI A. SORBI C. GALLESI R. BUCCIONI, Michela MARUCCI, Gabriella DE STEFANI C. CILIA A. BRASILI L. mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2009
Rivista:	CHEMMEDCHEM
Abstract:	Starting from compound 1, a previously reported a1D-adrenocep- tors antagonist, a new series of ligands acting at 5-HT1A serotonin receptor were identified through simple structure modifications. Among them (2,2-diphenyl-[1,3]oxathiolan-5-yl-methyl)-(3-phenylpropylamine (19) exhibits outstanding activity (pKi=8.72, pD2=7.67, E max=85) and selectivity (5-HT1A/α1D, 150), and represents an as yet unidentified 5-HT1A agonist scaffold.
Handle:	http://hdl.handle.net/11581/112247
Appare nelle tipologie:	Articolo

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