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

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Title Synthesis, Radiolabelling and Biodistribution of HYNIC-Tyr3
Octreotide: a Somatostatin Receptor Positive Tumour Imaging Agent
 
Creator Behera, Ashok
De, Kakali
Chandra, Susmita
Chattopadhyay, Sankha
Misra, Mridula
 
Subject Infectious Diseases and Immunology
 
Description 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.
 
Publisher —
 
Date 2011
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/1305/1/JOURNAL_OF_RADIOANALYTICAL_AND_NUCLEAR_CHEMISTRY_290(_1)123%2D129;2011[35].pdf
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.
 
Relation http://dx.doi.org/10.1007/s10967-011-1156-1
http://www.eprints.iicb.res.in/1305/