Synthesis, labeling, formulation and quality control of 99mTc-Tricine-HYNIC-Tyr³-Octreotide, a peptide radiopharmaceutical for imaging Somatostatin receptor positive tumors [Persian]

Document Type: Original Article

Authors

1 Department of Radioisotope, Nuclear Research Center, AOEI, Tehran, Iran

2 Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

3 Department of Pharmacology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran

Abstract

Somatostatin analoges labeled with different radionuclides are able used for imaging and treatment of somatostatin receptor positive tumors. In this study Tyr³-Octreotide protected at lysine as an analoge of somatostatin was conjugated with bifunctional chelating agent 6-BOC-hydrazinopyridine-3-carboxylic acid (BOC-HYNIC) and after deprotecting of conjugate, purification was performed with preparative-RP-HPLC. The conjugated peptide was labeled with 99mTc and tricine as coligand. Radiolabelling efficiency, radiochemical purity, stability in human serum, internalization of receptor bound 99mTc-labeled peptide and biodistribution in normal mice were studied.

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