Journal of Radioanalytical and Nuclear Chemistry

, Volume 301, Issue 3, pp 847–861 | Cite as

Radiolabeled novel peptide for imaging somatostatin-receptor expressing tumor: synthesis and radiobiological evaluation

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Abstract

The aim of this study was to synthesis, a radiolabeled (99mTc) new somatostatin-analogue 6-hydrazinopyridine-3-carboxylic-acid (HYNIC)-Asn3-octreotate (99mTc-HYNIC-AATE), and to evaluate as a candidate for imaging somatostatin-receptor (SSTR)-positive tumors and also compare it with 99mTc-HYNIC-Tyr3-octreotide (99mTc-HYNIC-TOC). Synthesis was performed by Fmoc-solid-phase strategy and 99mTc labeled by SnCl2. Biodistribution and imaging properties of new radiopeptide were also studied in C6 tumor bearing rat. Radiolabeling was performed at high specific activities and it showed high binding-affinity for SSTR2. In biodistribution, radiopeptides have showed high and receptor-specific uptake in the SSTR2 positive organs, tumor with rapid renal excretion from non-target tissues. These results demonstrated that 99mTc-HYNIC-AATE is a new specific radioligand for scintigraphy of somatostatin-receptor-positive tumors.

Keywords

Somatostatin receptor HYNIC Octreotate 99mTc C6 tumor 
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Notes

Acknowledgments

Financial support in the form of Research Associateship (Dr. Kakali De) from the Indian Council of Medical Research (ICMR), New Delhi, India, is acknowledged. The authors also gratefully acknowledge Prof. Siddhartha Roy, Director, CSIR-Indian Institute of Chemical Biology, Kolkata, India for infrastructure support of this work.

Supplementary material

10967_2014_3199_MOESM1_ESM.doc (397 kb)
Supplementary material 1 (DOC 397 kb)

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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2014

Authors and Affiliations

  1. 1.Department of Infectious Diseases and Immunology (Nuclear Medicine Division)Council of Scientific and Industrial Research (CSIR)-Indian Institute of Chemical Biology (IICB)KolkataIndia
  2. 2.Regional Radiation Medicine CentreVariable Energy Cyclotron CentreKolkataIndia

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