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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
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Sci. Pharm. 2014, 82(1), 29-42; (registering DOI)

Synthesis and Evaluation of [67Ga]-AMD3100: A Novel Imaging Agent for Targeting the Chemokine Receptor CXCR4

Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran
Department of Nuclear Pharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
Radiation Application Research School, Nuclear Science and Technology Research Institute, Tehran, 11365-3486, Iran
Clinic of Nuclear Medicine, University Medical Centre Mainz, Langenbeckstr. 1, D-55131 Mainz, Germany
Author to whom correspondence should be addressed.
Received: 12 March 2013 / Accepted: 12 September 2013 / Published: 12 September 2013
PDF [519 KB, uploaded 26 September 2016]


In order to develop a possible C-X-C chemokine receptor type 4 (CXCR4) imaging agent for oncological scintigraphy, [67Ga]-labeled 1,1′-[1,4-Phenylene-bis(methylene)]bis(1,4,8,11-tetraazacyclotetradecane) ([67Ga]-AMD3100) was prepared by using [67Ga]GaCl3 and AMD-3100 for 2 h at 50 °C (radiochemical purity: >95% ITLC, >99% HPLC, specific activity: 1800–2000 TBq/mmol) in acetate buffer. The stability of the complex was checked in the presence of human serum (37 °C) and in the final formulation for four days. The biodistribution of the labeled compound in the vital organs of wild type Sprague-Dawley rats was determined and compared with that of the free Ga3+ cation up to 48 h. Considering the spleen as the target organ, the best target:non target ratios were obtained 48 h post-injection (spleen:blood ratio; 14.5 and spleen:muscle ratio; 88.4). Initial SPECT images and biodistribution results in the wild type rats matched each other and demonstrated rapid washout of the tracer from the urinary tract. SPECT images in human breast carcinoma-bearing mice demonstrated a detectable tumor uptake in 48 h post-injection.
Keywords: Gallium-67; CXCR4; Biodistribution; SPECT; Breast carcinoma Gallium-67; CXCR4; Biodistribution; SPECT; Breast carcinoma
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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AGHANEJAD, A.; JALILIAN, A.R.; FAZAELI, Y.; ALIREZAPOOR, B.; POULADI, M.; BEIKI, D.; MAUS, S.; KHALAJ, A. Synthesis and Evaluation of [67Ga]-AMD3100: A Novel Imaging Agent for Targeting the Chemokine Receptor CXCR4 . Sci. Pharm. 2014, 82, 29-42.

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