Synthesis of neurotensin(8-13)-phosphopeptide heterodimers via click chemistry

Two neurotensin(8-13)-containing peptide heterodimers were prepared via copper(I)-mediated click chemistry. The resulting peptide dimers could be obtained in 28-31% yield after HPLC purification. Neurotensin( 8-13)-containing peptide dimers were used in an in vitro binding assay to determine binding affinity towards the neurotensin receptor-1 (NTR1). The determined IC₅₀ values of 8.3 µM and 0.7 µM indicate only very low binding affinity of the neurotensin(8-13)-containing peptide heterodimers towards the NTR1.