Radiochemical Evaluation of New 99mTc-labelled Bombesin Derivatives with Tripeptidic (Ser- Ser - Ser) and (Gly-Gly-Gly) Spacer for Targeting GRP Receptor Positive-tumors - Journal of Mazandaran University of Medical Sciences
Volume 25, Number 129 (10-2015)                   J Mazandaran Univ Med Sci 2015, 25(129): 70-80 | Back to browse issues page


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Sadeghzadeh N, Pishsaraie H, Ghasemi Y, Emrarian I. Radiochemical Evaluation of New 99mTc-labelled Bombesin Derivatives with Tripeptidic (Ser- Ser - Ser) and (Gly-Gly-Gly) Spacer for Targeting GRP Receptor Positive-tumors. J Mazandaran Univ Med Sci. 2015; 25 (129) :70-80
URL: http://jmums.mazums.ac.ir/article-1-6252-en.html

Abstract:   (5576 Views)
Background and purpose: Bombesin shows very high-affinity for the Gasterin releasing peptide (GRP) receptors which are over expressed in different human tumors such as breast and prostate. The aim of this study was to identify a new bombesin derivative labeled with 99mTc via HYNIC that might be used as a noninvasive tool for diagnosis of GRP receptor expressing tumors. Materials and methods: Prepared bombein derivatives were radiolabeled with 99mTc at 100 °C for 10 min by exchange method and radiochemical analysis was performed using ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37 °C and saline for up to 24 h. Results: [99mTc-EDDA/tricin/HYNIC-(Ser)3-D-Phe13]BN(7-14) and [99mTc-EDDA/tricin/ HYNIC-(Gly)3-D-Phe13]BN (7-14) were obtained with radiochemical purities of >95%. Results of in-vitro studies demonstrated a high stability in serum and saline. Conclusion: Radiolabeling of this novel conjugates with 99mTc were easily performed using exchange labeling. The prepared 99mTc-HYNIC-BN conjugates demonstrated some potential as site-directed diagnostic radiopharmaceuticals. Therefore, more in vivo studies are required.
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Type of Study: Research(Original) | Subject: Nuclear pharmacy

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