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Preparation and characterization of a novel Al(18)F-NOTA-BZA conjugate for melanin-targeted imaging of malignant melanoma.
Chang, Chih-Chao; Chang, Chih-Hsien; Lo, Yi-Hsuan; Lin, Ming-Hsien; Shen, Chih-Chieh; Liu, Ren-Shyan; Wang, Hsin-Ell; Chen, Chuan-Lin.
Afiliação
  • Chang CC; Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155, Li-Nong St., Sec. 2, Pei-tou, Taipei 11221, Taiwan.
  • Chang CH; Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155, Li-Nong St., Sec. 2, Pei-tou, Taipei 11221, Taiwan; Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan, Taiwan.
  • Lo YH; Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155, Li-Nong St., Sec. 2, Pei-tou, Taipei 11221, Taiwan.
  • Lin MH; Department of Nuclear Medicine, Taipei City Hospital, Zhongxiao Branch, Taipei, Taiwan.
  • Shen CC; Department of Nuclear Medicine, Cheng Hsin General Hospital, Taipei, Taiwan.
  • Liu RS; Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155, Li-Nong St., Sec. 2, Pei-tou, Taipei 11221, Taiwan; Molecular and Genetic Imaging Core/Taiwan Mouse Clinic, National Comprehensive Mouse Phenotyping and Drug Testing Center, Taipei, Taiwan; National P
  • Wang HE; Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155, Li-Nong St., Sec. 2, Pei-tou, Taipei 11221, Taiwan. Electronic address: hewang@ym.edu.tw.
  • Chen CL; Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, No. 155, Li-Nong St., Sec. 2, Pei-tou, Taipei 11221, Taiwan. Electronic address: clchen2@ym.edu.tw.
Bioorg Med Chem Lett ; 26(16): 4133-9, 2016 08 15.
Article em En | MEDLINE | ID: mdl-27445169
ABSTRACT
Melanin is an attractive target for the diagnosis and treatment of malignant melanoma. Previous studies have demonstrated the specific binding ability of benzamide moiety to melanin. In this study, we developed a novel (18)F-labeled NOTA-benzamide conjugate, Al(18)F-NOTA-BZA, which can be synthesized in 30min with a radiochemical yield of 20-35% and a radiochemical purity of >95%. Al(18)F-NOTA-BZA is highly hydrophilic (logP=-1.96) and shows good in vitro stability. Intravenous administration of Al(18)F-NOTA-BZA in two melanoma-bearing mouse models revealed highly specific uptake in B16F0 melanotic melanoma (6.67±0.91 and 1.50±0.26%ID/g at 15 and 120min p.i., respectively), but not in A375 amelanotic melanoma (0.87±0.21 and 0.24±0.09%ID/g at 15 and 120min p.i., respectively). The clearance from most normal tissues was fast. A microPET scan of Al(18)F-NOTA-BZA-injected mice also displayed high-contrast tumor images as compared with normal organs. Owing to the favorable in vivo distribution of Al(18)F-NOTA-BZA after intravenous administration, the estimated absorption dose was low in all normal organs and tissues. The melanin-specific binding ability, sustained tumor retention, fast normal tissues clearance and thelow projected human dosimetry supported that Al(18)F-NOTA-BZA is a very promising melanin-specific PET probe for melanin-positive melanoma.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzamidas / Melanoma Experimental / Compostos Radiofarmacêuticos / Tomografia por Emissão de Pósitrons / Melaninas Limite: Animals / Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzamidas / Melanoma Experimental / Compostos Radiofarmacêuticos / Tomografia por Emissão de Pósitrons / Melaninas Limite: Animals / Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article