Synthesis and characterization of a (68)Ga-labeled N-(2-diethylaminoethyl)benzamide derivative as potential PET probe for malignant melanoma

• Published in: Bioorganic & medicinal chemistry Vol. 20; no. 16; pp. 4915 - 4920
• Main Authors: Kim, Hee-Jung, Kim, Dong-Yeon, Park, Jeong-Hoon, Yang, Seung-Dae, Hur, Min-Goo, Min, Jung-Joon, Yu, Kook-Hyun
• Format: Journal Article
• Language: English
• Published: England 15.08.2012
• Subjects: Animals; Benzamides - chemical synthesis; Benzamides - chemistry; Cell Line, Tumor; Disease Models, Animal; Gallium Radioisotopes; Melanoma, Experimental - diagnosis; Mice; Positron-Emission Tomography; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - pharmacokinetics
• ISSN: 1464-3391
• DOI: 10.1016/j.bmc.2012.06.047

Radiolabeled benzamides have been reported to be attractive agents for targeting malignant melanoma as they bind melanin and display high accumulation in melanoma cells. Herein, we report the synthesis and bioevaluation of a novel (68)Ga-labeled benzamide as a potential PET agent for malignant melanoma. The novel radiotracer was synthesized in good radiochemical yields (80% decay corrected yield) and high specific radioactivity (10 GBq/μmol). Cellular uptake of (68)Ga-SCN-NOTA-BZA was significantly higher in B16F10 cells (mouse melanoma) treated with L-tyrosine. Biodistribution and micro-PET studies of (68)Ga-SCN-NOTA-BZA in B16F10-bearing mice showed selective uptake into the tumor. The radiotracer was cleared via renal excretion without further metabolism. These results demonstrate that (68)Ga-SCN-NOTA-BZA is a potential PET probe for malignant melanoma.