1. Synthesis and Preclinical Characterization of [18F]FPBZA: A Novel PET Probe for Melanoma
- Author
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Shyh Jen Wang, Chih Chieh Shen, Shih Yen Wu, Wuu Jyh Lin, Yen Chen Lo, Shih Pin Huang, Hsin Ell Wang, and Ren-Shyan Liu
- Subjects
Pathology ,medicine.medical_specialty ,Article Subject ,Melanoma, Experimental ,lcsh:Medicine ,Inflammation ,Tumor cells ,General Biochemistry, Genetics and Molecular Biology ,Lesion ,Mice ,chemistry.chemical_compound ,Fluorodeoxyglucose F18 ,medicine ,Animals ,Humans ,Tissue Distribution ,Amelanotic melanoma ,Benzamide ,Lung ,General Immunology and Microbiology ,medicine.diagnostic_test ,business.industry ,Melanoma ,lcsh:R ,General Medicine ,medicine.disease ,medicine.anatomical_structure ,chemistry ,Positron emission tomography ,Positron-Emission Tomography ,Benzamides ,Cancer research ,Radiopharmaceuticals ,medicine.symptom ,business ,Research Article - Abstract
Introduction. Benzamide can specifically bind to melanoma cells. A18F-labeled benzamide derivative, [18F]N-(2-diethylaminoethyl)-4-[2-(2-(2-fluoroethoxy) ethoxy)ethoxy]benzamide ([18F]FPBZA), was developed as a promising PET probe for primary and metastatic melanoma.Methods. [18F]FPBZA was synthesized via a one-step radiofluorination in this study. The specific uptake of [18F]FPBZA was studied in B16F0 melanoma cells, A375 amelanotic melanoma cells, and NB-DNJ-pretreated B16F0 melanoma cells. The biological characterization of [18F]FPBZA was performed on mice bearing B16F0 melanoma, A375 amelanotic melanoma, or inflammation lesion.Results. [18F]FPBZA can be prepared efficiently with a yield of 40โ50%. The uptake of [18F]FPBZA by B16F0 melanoma cells was significantly higher than those by A375 tumor cells and NB-DNJ-pretreated B16F0 melanoma cells. B16F0 melanoma displayed prominent uptake of [18F]FPBZA at 2 h (7.81±0.82 %ID/g), compared with A375 tumor and inflammation lesion (3.00±0.71and1.67±0.56 %ID/g, resp.). [18F]FPBZA microPET scan clearly delineated B16F0 melanoma but not A375 tumor and inflammation lesion. In mice bearing pulmonary metastases, the lung radioactivity reached4.77±0.36 %ID/g at 2 h (versus1.16±0.23 %ID/g in normal mice).Conclusions. Our results suggested that [18F]FPBZA PET would provide a promising and specific approach for the detection of primary and metastatic melanoma lesions.
- Published
- 2014