From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor

…, O Cruz-Lopez, MA Tabrizi, AR Moorman…

Index: Romagnoli, Romeo; Baraldi, Pier Giovanni; Carrion, Maria Dora; Cara, Carlota Lopez; Preti, Delia; Cruz-Lopez, Olga; Tabrizi, Mojgan Aghazadeh; Moorman, Allan R.; Gessi, Stefania; Fogli, Eleonora; Sacchetto, Valeria; Borea, Pier Andrea Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3706 - 3715

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Citation Number: 11

Abstract

The characterization of the native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtype-selective antagonists with a “druglike” profile. However, a tyrosine derivative named KN-62 exhibits selective P2X7 receptor-blocking properties. As a molecular simplification of KN-62, the present study was designed to evaluate the functional antagonistic properties of a novel series of glycine derivatives characterized by the ...