Synthesis, Radiolabelling and Biodistribution of HYNIC-Tyr3 Octreotide: a Somatostatin Receptor Positive Tumour Imaging Agent

Behera, Ashok and De, Kakali and Chandra, Susmita and Chattopadhyay, Sankha and Misra, Mridula (2011) Synthesis, Radiolabelling and Biodistribution of HYNIC-Tyr3 Octreotide: a Somatostatin Receptor Positive Tumour Imaging Agent. Journal of Radioanalytical and Nuclear Chemistry, 290 (1). pp. 123-129.

[img]

PDF
Restricted to IICB Scientists only

Download (346Kb) | Request a copy

    Abstract

    In vivo imaging of tumours using radiolabelled somatostatin (SST) analogues has become an accepted clinical tool in oncology. HYNIC-Tyr3 octreotide and Tyr3 octreotide were synthesized by FMOC solid-phase peptide synthesis using a semi-automated synthesizer. These were analyzed and purified by RP-HPLC, mass spectroscopy, IR spectroscopy, 1H NMR and 13C NMR. The prochelator 6-BOC-HYNIC was also synthesised and characterised indigenously. HYNIC-Tyr3 octreotide was labelled with 99mTc using Tricine and EDDA as coligand by SnCl2 method. Labelling with 99mTc was performed at 100 �C for 15 min and radiochemical analysis by ITLC and HPLC methods. The radiochemical purity of the complex was over 98% and log p value was found to be -1.27 ± 0.12. The stability of radiolabelled peptide complex was checked at 37 �C up to 24 h. Blood clearance and protein-binding study was also performed. In vivo biodistribution studies in rat showed uptake of 99mTc-HYNIC-TOC in kidney than any other organs. The blood clearance was faster with rapid excretion through kidneys and relatively low uptake in liver.

    Item Type: Article
    URI: http://www.eprints.iicb.res.in/id/eprint/1305
    Subjects: Infectious Diseases and Immunology
    Divisions: Indian Institute of Chemical Biology
    Depositing User: Ms Sutapa Ganguly
    Date Deposited: 23 Jan 2012 12:37
    Last Modified: 25 Jan 2012 11:28
    Official URL: http://dx.doi.org/10.1007/s10967-011-1156-1
    Links:

    Actions (login required)

    View Item