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The successful peptide receptor imaging of tumors, as exemplified for somatostatin receptors, is based on the overexpression of peptide receptors in selected tumors and the high-affinity binding to these tumors of agonist radioligands that are subsequently internalized into the tumor cells in which they accumulate. Although in vitro studies have shown ample evidence that the ligand-receptor complex is internalized, in vivo evidence of agonist-induced internalization of peptide receptors, such as somatostatin receptors, is missing.

Highly Efficient In Vivo Agonist-Induced Internalization of sst2 Receptors in Somatostatin Target Tissues

Highly Efficient In Vivo Agonist-Induced Internalization of sst₂ Receptors in Somatostatin Target Tissues