Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor

…, G Bastanzio, M Sbraccia, C Mustazza, I Sestili

Index: Del Giudice, Maria Rosaria; Borioni, Anna; Bastanzio, Giuditta; Sbraccia, Maria; Mustazza, Carlo; Sestili, Isabella European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1207 - 1221

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Citation Number: 7

Abstract

Bivalent ligands constituted by two identical pharmacophores structurally related to the Nociceptin Opioid Receptor (NOPr) antagonist JTC-801 were synthesized and their binding affinities for NOPr were evaluated. The novel ligands are formed by two modified JTC-801 units linked by di-iminic and di-aminic spacers with length ranging from three to ten methylene units. Moreover, the synthesis and the pharmacological characterization were ...