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.
(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenyl-propyl)-amine: a Potent and Selective 5-HT1A Receptor Agonist
BUCCIONI, Michela;MARUCCI, Gabriella;
2009-01-01
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.File in questo prodotto:
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