New freeze-dried kit for diagnosis of Bombesin receptor expressing tumors
- سال انتشار: 1389
- محل انتشار: مجله پزشکی هسته ای ایران، دوره: 18، شماره: 2
- کد COI اختصاصی: JR_IRJNM-18-2_002
- زبان مقاله: انگلیسی
- تعداد مشاهده: 324
نویسندگان
Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran
Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran
Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran
Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran
چکیده
Introduction: It has been shown that some primary human tumors and their metastases, including prostate and breast tumors, over-express gastrin-releasing peptide (GRP) receptors. Bombesin is a neuropeptide with a high affinity for these GRP receptors. The purpose of this study was to prepare and evaluate the characteristics of a new Freeze-dried kit, [6-hydrazinopyridine-3-carboxylic acid (HYNIC)]-GABA-Bombesin [7-14] NH2 designed for the labeling with 99mTc using tricine and EDDA as coligand. Methods: Synthesis was performed on a solid phase using a standard Fmoc strategy and HYNIC precursor coupled at the N-terminus. Purified peptide conjugate was labeled with 99mTc at 100°C for 10 min. Radiochemical analysis involved ITLC and high-performance liquid chromatography methods. Peptide conjugate stability and affinity to human serum was challenged for 24 hours. The internalization rate was studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in rats. Results: Radiolabeling was performed at high specific activities, and radiochemical purity was > 98%. The stability of radiolabeled peptide in human serum was excellent. In vitro studies showed > 14% of activity was specific internalized into PC-3 cells up to 4 h. After injection into rat biodistribution data showed a rapid blood clearance, with renal excretion and specific binding towards GRP receptor-positive tissues such as pancreas (1.15±0.19% ID/g after 4 h). Conclusion: [99mTc-HYNIC]-GABA-Bombesin [7-14] NH2 showed favorable radiochemical and biological characteristics which make our new designed labeled peptide conjugate as a very suitable agent for diagnostic purposes in malignant tumors.کلیدواژه ها
Bombesin, HYNIC, Freeze-dried Kit, GRP receptors, Tumorاطلاعات بیشتر در مورد COI
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