A 99mTc‐tricine‐HYNIC‐labeled peptide targeting the neurotensin receptor for single‐photon imaging in malignant tumors. (7th January 2014)

• Record Type: Journal Article
• Authors: Erfani, Mostafa; Zarrabi Ahrabi, Nakisa; Shafiei, Mohammad; Shirmardi, Seyed Pezhman
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 57:Number 3(2014)
• Page Start: 125
• Page End: 131
• Publication Date: 2014-01-07
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3176
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>In this study, a new neurotensin (NT) analog was labeled with ^99mTc via HYNIC chelator and tricine as coligand and investigated further.</p> <p>An NT (7–13) analog was prepared, and labeling with ^99mTc was performed. The internalization rate and biodistribution of radiopeptide were studied in HT‐29 cells and nude mice bearing tumor, respectively.</p> <p>Radiolabeling with ^99mTc was performed at high specific activities (54 MBq/nmol) with an acceptable labeling yield (&gt;95%). <italic>In vitro</italic> cell line studies showed a specific internalization uptake up to 13.23 ± 0.45% during 4 h which was blocked in the presence of excess cold peptide to 0.83 ± 0.15%. In biodistribution studies, uptake was observed in NT receptor‐positive organs so that after 1 h the uptakes in mouse intestine and tumor were 1.23 ± 0.16% ID/g and 1.12 ± 0.11% ID/g, respectively. In animals co‐injected with excess cold peptide, reduction uptake in tumor and intestines were 73% (1.10% vs. 0.29% ID/g at 4 h) and 61% (1.22% vs. 0.47% ID/g at 4 h) respectively. Predominant renal excretion pathway with a highest accumulation of activity in bladder was observed for this radiopeptide. This radiolabeled peptide could be a candidate for detection of NT positive tumors.</p> </abstract>