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Nuclear medicine and biology

Radionuclide imaging of small-cell lung cancer (SCLC) using 99mTc-labeled neurotensin peptide 8-13.


PMID 16720242

Abstract

To prepare 99m technetium (99mTc)-labeled neurotensin (NT) peptide and to evaluate the feasibility of imaging oncogene NT receptors overexpressed in human small-cell lung cancer (SCLC) cells. The NT analogue (Nalpha-His)Ac-NT(8-13) was synthesized such that histidine was attached at the N-terminus. The analogue was labeled with [99mTc(H2O)3(CO)3] at pH 7. 99mTc-(Nalpha-His)Ac-NT(8-13) in vitro stability was determined by challenging it with 100 times the molar excess of DTPA, human serum albumin (HSA) and cysteine. The affinity, 99mTc-(Nalpha-His)Ac-NT(8-13) binding to SCLC cell line NCI-H446, was studied in vitro. Biodistribution and imaging with 99mTc-(Nalpha-His)Ac-NT(8-13) were performed at 4 and 12 h postinjection, and tissue distribution and imaging after receptor blocking were carried out at 4 h in nude mice bearing human SCLC tumor. Blood clearance was determined in normal mice. The affinity constant (Kd) of 99mTc-(Nalpha-His)Ac-NT(8-13) to SCLC cells was 0.56 nmol/L. When challenged with 100 times the molar excess of DTPA, HSA or cysteine, more than 97+/-1.8% radioactivity remained as 99mTc-(Nalpha-His)Ac-NT(8-13). Tumor-to-muscle ratio was 3.35+/-1.01 at 4 h and 4.20+/-1.35 at 12 h postinjection. The excretory route of 99mTc-(Nalpha-His)Ac-NT(8-13) was chiefly through the renal pathway. In the receptor-blocking group treated with unlabeled (Nalpha-His)Ac-NT(8-13), tumor-to-muscle ratio at 4 h was 1.25+/-0.55. The results suggest that 99mTc-(Nalpha-His)Ac-NT(8-13) specifically binds to the SCLC cells and made 99mTc-(Nalpha-His)Ac-NT(8-13) a desirable compound for further studies in planar or SPECT imaging of oncogene receptors overexpressed in SCLC cells.

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N5266
Neurotensin Fragment 8-13 acetate salt, ≥97% (HPLC)
C38H64N12O8