Solid Phase Synthesis of Oxytocin Analogues Conjugated to Polyamino Polycarboxylic Ligands

Abstract

An easy solid phase synthesis of oxytocin analogues conjugated to polyaminopolycarboxylic ligand, such as diethylenetriaminepentaacetic acid (DTPA) and tetraazacyclododecanetetraacetic acid (DOTA) is reported. These new products can be labeled with suitable radiometals (e.g. 90Y, 111In, 177Lu), giving rise to radiopharmaceuticals with potential application in imaging and/or therapy of tumors over-expressing oxytocin receptors. Keywords: Oxytocin, solid phase peptide synthesis, targeting, DOTA, DTPA, radiolabeled peptides