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(2,2‐Diphenyl‐[1,3]oxathiolan‐5‐ylmethyl)‐(3‐phenyl‐propyl)‐amine: a Potent and Selective 5‐HT 1A Receptor Agonist
Author(s) -
Franchini Silvia,
Tait Annalisa,
Prandi Adolfo,
Sorbi Claudia,
Gallesi Rossella,
Buccioni Michela,
Marucci Gabriella,
De Stefani Carla,
Cilia Antonio,
Brasili Livio
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800276
Subject(s) - agonist , chemistry , amine gas treating , selectivity , partial agonist , stereochemistry , 5 ht receptor , antagonist , serotonin , receptor , biochemistry , organic chemistry , catalysis
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.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.
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