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: | |
Data di pubblicazione: | 2009 |
Rivista: | |
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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