Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2018 Feb 1;9(3):454-459.
doi: 10.1039/c7md00607a. eCollection 2018 Mar 1.

Automated synthesis of [68Ga]oxine, improved preparation of 68Ga-labeled erythrocytes for blood-pool imaging, and preclinical evaluation in rodents

Stephen Thompson  1 , Melissa E Rodnick  1 , Jenelle Stauff  1 , Janna Arteaga  1 , Timothy J Desmond  1 , Peter J H Scott  1 , Benjamin L Viglianti  1   2
Affiliations

Automated synthesis of [68Ga]oxine, improved preparation of 68Ga-labeled erythrocytes for blood-pool imaging, and preclinical evaluation in rodents

Stephen Thompson et al. Medchemcomm. .

Abstract

Radiolabeled erythrocytes have multiple applications in nuclear medicine, including blood pool imaging. Historically they have been labeled with SPECT radionuclides. A PET blood pool imaging agent is highly desirable as it would improve clinical applications with better image quality and resolution, higher sensitivity, and dynamic scanning capabilities. With the coming of age of modern 68Ge/68Ga generator systems, gallium-68 is now widely accessible. In this paper we describe an updated method for the preparation of 68Ga-labeled erythrocytes and their preliminary use in rodent blood pool imaging. A novel automated synthesis of [68Ga]oxine using a 68Ga/68Ge generator and automated synthesis module is reported. [68Ga]Oxine was synthesized in 50 ± 5% (n = 3) non-decay corrected radiochemical yield and >99% radiochemical purity. Rat and human erythrocytes were successfully labeled with the complex in 42% RCY, and the 68Ga-labeled erythrocytes have been shown to clearly image the blood pool in a healthy rat. Human erythrocytes labelled with [68Ga]oxine were shown to be viable up to 2 hours post-labelling, and washout of the radiolabel was minimal up to 1 hour post-labelling. Further optimization of the labeling method to translate for use in human cardiac and oncologic blood pool PET imaging studies, is underway.

PubMed Disclaimer

Figures

Scheme 1
Scheme 1. Synthesis of [68Ga]oxine.
Fig. 1
Fig. 1. A. Sagittal (sag) and coronal (cor) summed (0–55 min) microPET image of washed 68Ga-labeled erythrocytes in a rat, showing high uptake in the heart and descending aorta/vena cava, and minimal liver uptake. B. Time activity curve (n = 3) showing peak SUV of 10.5 in the heart and 4 in the liver, and equilibrium SUV of 9 in the heart and 3.4 in the liver.
Fig. 2
Fig. 2. A. Sagittal (sag) and coronal (cor) summed (0–55 min) micro PET image of [68Ga]oxine in a rat, showing high uptake in the liver, but minimal cardiac uptake. B. Time activity curve (n = 2) showing peak SUV of 7 in the liver and 9 in the heart, and equilibrium SUV of 3.7 in the heart 6.5 in the liver.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Love C., Palestro C. J. J. Nucl. Med. Technol. 2004;32:47. - PubMed
    1. McDonald M. A., Ziessman H. A. Appl. Radiol. 2016;45:19.
    1. Fatima N., uz Zaman M., Hashmi A., Kamal S., Hameed A. Nucl. Med. Commun. 2011;32:381. - PubMed
    1. Xie B.-Q., Tian Y.-Q., Zhang J., Zhao S.-H., Yang M.-F., Guo F., Wang D.-Y., Wei H.-X., Chu K.-W., He Z.-X. J. Nucl. Med. 2012;53:584. - PubMed
    1. Chernov V. I., Kravchuk T. L., Zelchan R. V., Goldberg V. E. Kardiologiia. 2015;55:5. - PubMed