[113m In]In-AMBA: A Novel Diagnostic Agent for SPECT Imaging of GRPR-Expressing Tumors
[113m In]In-AMBA: A Novel Diagnostic Agent for SPECT Imaging of GRPR-Expressing Tumors
Mohammad Moazami-Ashtiani(Institute of Biochemistry and Biophysics, University of Tehran, Tehran 1417614411, Iran); Saeed Rajabifar(Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box 14395-836, Tehran, Iran); Samaneh Zolghadri(Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box 14395-836, Tehran, Iran); Hassan Yousefnia(Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box 14395-836, Tehran, Iran)
59권 2호, 125~134쪽
초록
Purpose Gastrin-releasing peptide receptor (GRPR), a member of the bombesin G-protein-coupled receptor family, is introducedas the promising target for the diagnosis and therapy of various tumors. This study aimed to develop a novel diagnosticagent of [113mIn]In-AMBA for single photon emission computed tomography (SPECT) imaging of GRPR expressing tumors. Methods 113mIn was provided from an in-house made 113Sn/113mIn generator in the chloride form. [113mIn]In-AMBA wasprepared in the optimal conditions and the stability was checked in PBS buffer and human serum, Then the binding affinityand internalization of the radiolabeled compound were investigated in PC3 cell lines at 120 min. the biodistribution of theradiolabeled peptide was studied in normal rats. Results [113mIn]In-AMBA was prepared with radiochemical purity (RCP) > 98% under the optimal labeling conditions. Thecompound indicated significant stability in PBS buffer and human serum (> 95% at 180 min post preparation). High bindingaffinity (51% at 60 min) and internalization (64% at 120 min) of the radiolabeled compound towards PC3 cell lines were alsoobserved. The major accumulation of the compound was seen in kidneys, and other GRPR-expressing tissues. Conclusion The biodistribution of the labeled compound in normal rats indicated rapid elimination of the complex fromthe blood, and considerable accumulation in the GRPR-expressing organ of pancreas, in complete agreement with similarlabeled compounds. [113mIn]In-AMBA can be a suitable candidate for SPECT imaging of GRPR-expressed tumors.
Abstract
Purpose Gastrin-releasing peptide receptor (GRPR), a member of the bombesin G-protein-coupled receptor family, is introducedas the promising target for the diagnosis and therapy of various tumors. This study aimed to develop a novel diagnosticagent of [113mIn]In-AMBA for single photon emission computed tomography (SPECT) imaging of GRPR expressing tumors. Methods 113mIn was provided from an in-house made 113Sn/113mIn generator in the chloride form. [113mIn]In-AMBA wasprepared in the optimal conditions and the stability was checked in PBS buffer and human serum, Then the binding affinityand internalization of the radiolabeled compound were investigated in PC3 cell lines at 120 min. the biodistribution of theradiolabeled peptide was studied in normal rats. Results [113mIn]In-AMBA was prepared with radiochemical purity (RCP) > 98% under the optimal labeling conditions. Thecompound indicated significant stability in PBS buffer and human serum (> 95% at 180 min post preparation). High bindingaffinity (51% at 60 min) and internalization (64% at 120 min) of the radiolabeled compound towards PC3 cell lines were alsoobserved. The major accumulation of the compound was seen in kidneys, and other GRPR-expressing tissues. Conclusion The biodistribution of the labeled compound in normal rats indicated rapid elimination of the complex fromthe blood, and considerable accumulation in the GRPR-expressing organ of pancreas, in complete agreement with similarlabeled compounds. [113mIn]In-AMBA can be a suitable candidate for SPECT imaging of GRPR-expressed tumors.
- 발행기관:
- 대한핵의학회
- 분류:
- 핵의학