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Development of a 68Ga-peptide tracer for PET GnRH1-imaging

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Annals of Nuclear Medicine Aims and scope Submit manuscript

An Erratum to this article was published on 08 June 2016

Abstract

Objective

Total synthesis, quality control and preclinical evaluation of [68Ga]-DOTA-triptorelin ([68Ga]-DOTA-TRP) is reported as a possible PET radiotracer for GnRH receptor imaging.

Methods

DOTA-TRP was totally synthesized in two steps and after characterization went through radiolabelling optimization studies followed by tracer stability. The biodistribution of the tracer in normal male rats and 4T1 tumour-bearing mice was performed in 120 min after i.v. injection.

Results

The peptide and the conjugates were synthesized with >95 % chemical purity. [68Ga]-DOTA-TRP complex was prepared in high radiochemical purity (>99 %, ITLC, HPLC) and specific activity of 1400–2100 MBq/nM at 95 °C using 40–60 μg of the peptide in 5–7 min followed by solid phase purification. The IC50 [nM] DOTA-TRP was comparable to the intact peptide, 0.11 ± 0.01 and 0.22 ± 0.05, respectively. The biodistribution of the tracer demonstrated kidney, stomach, and testes significant uptake, all in accordance with GnRH receptor ligands. Significant tumour uptake was observed in 4T1 tumour-bearing female mice 30–120 min post-injection with tumour:blood and tumour:muscle ratios of 28 and >50 in 60 min, respectively. Kidney is rapidly washed from the tracer. [68Ga]-DOTA-TRP can be proposed as a possible tracer for GnRH-R imaging studies.

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Acknowledgements

We acknowledge the financial support of Iran National Science Foundation (INSF) for conducting this research project for development of Ga-68-labelled peptides (Under 93035935). The authors wish to thank Mr. M. Mazidi for performing animal tests as well as Mr E. Moadi for HPLC experiments.

Sources of funding

This work has been in part supported by Iran National Science Foundation (INSF) for development of Ga-68-labelled peptide (Under 93035935).

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Authors and Affiliations

  1. Department of Chemistry, Faculty of Science, Arak Branch, Islamic Azad University, Arak, Iran

    Masoumeh Zoghi & Ali Niazi

  2. Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran

    Amir R. Jalilian, Fariba Johari-daha & Behrouz Alirezapour

  3. Peptide Chemistry Research Center, K. N. Toosi University of Technology, Tehran, Iran

    Saeed Ramezanpour

Authors
  1. Masoumeh Zoghi
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  2. Amir R. Jalilian
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  3. Ali Niazi
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  4. Fariba Johari-daha
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  5. Behrouz Alirezapour
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Correspondence to Amir R. Jalilian.

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Zoghi, M., Jalilian, A.R., Niazi, A. et al. Development of a 68Ga-peptide tracer for PET GnRH1-imaging. Ann Nucl Med 30, 400–408 (2016). https://doi.org/10.1007/s12149-016-1074-y

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  • DOI: https://doi.org/10.1007/s12149-016-1074-y

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