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

نویسندگان

  • Abbas Shafiee Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  • Gholamali Shabani Department of Radioisotope, Nuclear Research Center, AOEI, Tehran, Iran
  • Mohammad Hossein Babaei Department of Radioisotope, Nuclear Research Center, AOEI, Tehran, Iran
  • Mohannad Rabbani Department of Pharmacology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran
  • Mostafa Gandomkar Department of Radioisotope, Nuclear Research Center, AOEI, Tehran, Iran
  • Reza Najafi Department of Radioisotope, Nuclear Research Center, AOEI, Tehran, Iran
  • Seyed Esmail Sadatebrahimi Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
چکیده مقاله:

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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عنوان ژورنال

دوره 11  شماره 1

صفحات  23- 28

تاریخ انتشار 2003-11-01

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