Synthesis, Radiolabelling and Biodistribution of HYNIC-Tyr(3) Octreotide: a Somatostatin Receptor Positive Tumour Imaging Agent
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
View Archive Info| Field | Value | |
| Title |
Synthesis, Radiolabelling and Biodistribution of HYNIC-Tyr(3) Octreotide: a Somatostatin Receptor Positive Tumour Imaging Agent
|
|
| Creator |
Behera, Ashok
De, Kakali Chandra, Susmita Chattopadhyay, Sankha Misra, Mridula |
|
| Subject |
Structural Biology & Bioinformatics
|
|
| Description |
In vivo imaging of tumours using radiolabelled somatostatin (SST) analogues has become an accepted clinical tool in oncology. HYNIC-Tyr(3) octreotide and Tyr(3) 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, (1)H NMR and (13)C NMR. The prochelator 6-BOC-HYNIC was also synthesised and characterised indigenously. HYNIC-Tyr(3) octreotide was labelled with (99m)Tc using Tricine and EDDA as coligand by SnCl(2) method. Labelling with (99m)Tc was performed at 100 A degrees 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 +/- A 0.12. The stability of radiolabelled peptide complex was checked at 37 A degrees C up to 24 h. Blood clearance and protein-binding study was also performed. In vivo biodistribution studies in rat showed uptake of (99m)Tc-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 |
Kluwer
|
|
| Date |
2011
|
|
| Type |
Article
PeerReviewed |
|
| Format |
application/pdf
|
|
| Identifier |
http://www.eprints.iicb.res.in/11/1/fulltext1.pdf
Behera, Ashok and De, Kakali and Chandra, Susmita and Chattopadhyay, Sankha and Misra, Mridula (2011) Synthesis, Radiolabelling and Biodistribution of HYNIC-Tyr(3) Octreotide: a Somatostatin Receptor Positive Tumour Imaging Agent. Journal of Radioanalytical and Nuclear Chemistry, 290. pp. 123-129. |
|
| Relation |
http://dx.doi.org/10.1007/s10967-011-1156-1
http://www.eprints.iicb.res.in/11/ |
|