title: Synthesis and preclinical characterization of [18F]FPBZA: a novel PET probe for melanoma.
abstract: BACKGROUND
  Benzamide can specifically bind to melanoma cells. A 18F-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 40-50%. 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±0.71 and 1.67±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 reached 4.77±0.36%ID/g at 2 h (versus 1.16±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.
authors.affiliation: Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155 Li-Nong Street, Section 2, Pei-Tou, Taipei 11221, Taiwan.
authors.forename: Shih-Yen
authors.identifier: 0000-0002-2889-8989
authors.initials: SY
authors.lastname: Wu
authors.affiliation: Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155 Li-Nong Street, Section 2, Pei-Tou, Taipei 11221, Taiwan.
authors.forename: Shih-Pin
authors.initials: SP
authors.lastname: Huang
authors.affiliation: Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155 Li-Nong Street, Section 2, Pei-Tou, Taipei 11221, Taiwan.
authors.forename: Yen-Chen
authors.initials: YC
authors.lastname: Lo
authors.affiliation: Department of Nuclear Medicine, Faculty of Medicine, National Yang-Ming University, No. 155 Li-Nong Street, Section 2, Pei-Tou, Taipei 11221, Taiwan.
authors.forename: Ren-Shyan
authors.initials: RS
authors.lastname: Liu
authors.affiliation: Department of Nuclear Medicine, Faculty of Medicine, National Yang-Ming University, No. 155 Li-Nong Street, Section 2, Pei-Tou, Taipei 11221, Taiwan.
authors.forename: Shyh-Jen
authors.identifier: 0000-0001-6014-0484
authors.initials: SJ
authors.lastname: Wang
authors.affiliation: Institute of Nuclear Energy Research, Atomic Energy Council, No. 1000 Wenhua Road, Jiaan Village, Longtan, Taoyuan County 32546, Taiwan.
authors.forename: Wuu-Jyh
authors.identifier: 0000-0003-0330-7537
authors.initials: WJ
authors.lastname: Lin
authors.affiliation: Department of Nuclear Medicine, Cheng Hsin General Hospital, No. 45 Cheng Hsin Street, Pei-Tou, Taipei 11220, Taiwan.
authors.forename: Chih-Chieh
authors.initials: CC
authors.lastname: Shen
authors.affiliation: Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155 Li-Nong Street, Section 2, Pei-Tou, Taipei 11221, Taiwan.
authors.forename: Hsin-Ell
authors.identifier: 0000-0003-4818-4921
authors.initials: HE
authors.lastname: Wang
mesh_terms: D000818:Animals; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry; D019788:Fluorodeoxyglucose F18 / Q000138:chemical synthesis / Q000737:chemistry; D006801:Humans; D008546:Melanoma, Experimental / Q000175:diagnosis* / Q000473:pathology; D051379:Mice; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry; D014018:Tissue Distribution
chemical_list: D001549:Benzamides; D019275:Radiopharmaceuticals; D019788:Fluorodeoxyglucose F18; C037689:benzamide