Sci Pharm. 2008; 76: 637–651.

Synthesis and Preclinical Studies of [⁶¹Cu]-N-(2-hydroxyacetophenone)glycinate as a Possible PET Radiopharmaceutical

Amir R. JALILIAN ¹, Hamid SADEGHI ², Hassan ZANDI ³, Pejman ROWSHANFARZAD ¹, Kamaledin SHAFAII ¹, Mohsen KAMALI-DEHGHAN ¹, Javad GAROUSI ¹, Abbas MAJDABADI ¹, Mohammad B. TAVAKOLI ²

¹ Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), Karaj, P.O.Box: 31485-498, Iran.
² Department of Biomedical Physics and Engineering, School of Medicine, Isfahan University of Medical Sciences, Isfahan, Iran
³ Islamic Azad University, Science and Research Unit, P.O.Box: 14155-775, Tehran, Iran.

* Corresponding author. E-mail: ajalilian@nrcam.org (A. R. Jalilian).

Abstract

[⁶¹Cu]-N-(2-hydroxyacetophenone)glycinate ([⁶¹Cu]NHAG) was prepared using in house-made NHAG ligand and [⁶¹Cu]CuCl2 produced via the ^natZn(p,x)⁶¹Cu (180μA proton irradiation, 22MeV, 3.2h) and purified by a ion chromatography method. [⁶¹Cu]NHAG radiochemical purity was >98% and >99.9% by RTLC and HPLC methods respectively after purification by SPE. [⁶¹Cu]NHAG was administered into normal and tumor bearing mice followed by biodistribution studies up to 180 minutes. The best tumor accumulation was observed by animal sacrification after 120 min (tumor/muscle and tumor/blood ratios were 25.6 and 3.4 respectively). [⁶¹Cu]NHAG is a potential PET radiotracer for tumor imaging.

Keywords

Radiopharmaceuticals • Copper-61 • NHAG • Biodistribution • Fibrosarcoma

Received August 19^th, 2008 | Accepted September 14^th, 2008 | Published Online September 17^th, 2008

doi:10.3797/scipharm.0808-13