(2,2‐Diphenyl‐[1,3]oxathiolan‐5‐ylmethyl)‐(3‐phenyl‐propyl)‐amine: a Potent and Selective 5‐HT_1A Receptor Agonist

Abstract

Abstract A selective 5‐HT 1A receptor agonist : A new series of ligands acting at 5‐HT 1A serotonin receptor were identified. Among them (2,2‐diphenyl‐[1,3]oxathiolan‐5‐yl‐methyl)‐(3‐phenyl‐propyl)amine (shown) possesses outstanding activity (p K i =8.72, pD 2 =7.67, E max =85) and selectivity (5‐HT 1A /α 1D >150), and represents a new 5‐HT 1A agonist chemotype. magnified image Starting from compound 1 , a previously reported α 1D ‐adrenoceptors antagonist, a new series of ligands acting at 5‐HT 1A serotonin receptor were identified through simple structure modifications. Among them (2,2‐diphenyl‐[1,3]oxathiolan‐5‐yl‐methyl)‐(3‐phenyl‐propyl)amine ( 19 ) exhibits outstanding activity (p K i =8.72, pD 2 =7.67, E max =85) and selectivity (5‐HT 1A /α 1D >150), and represents an as yet unidentified 5‐HT 1A agonist scaffold.