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Benzyl [(11)C]Hippurate as an Agent for Measuring the Activities of Organic Anion Transporter 3 in the Brain and Multidrug Resistance-Associated Protein 4 in the Heart of Mice.
Kikuchi, Tatsuya; Okamura, Toshimitsu; Okada, Maki; Ogawa, Masanao; Suzuki, Chie; Wakizaka, Hidekatsu; Yui, Joji; Fukumura, Toshimitsu; Gee, Antony D; Zhang, Ming-Rong.
Afiliação
  • Kikuchi T; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
  • Okamura T; Division of Imaging Sciences and Biomedical Engineering, King's College London , Fourth Floor Lambeth Wing, St. Thomas' Hospital, Lambeth Palace Road, London SE1 7EH, United Kingdom.
  • Okada M; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
  • Ogawa M; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
  • Suzuki C; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
  • Wakizaka H; SHI Accelerater Service Co. Ltd. , 5-9-1 Kitashinagawa, Shinagawa-ku, Tokyo 141-8686, Japan.
  • Yui J; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
  • Fukumura T; Preeminent Medical Photonics Education Research Center, Hamamatsu University School of Medicine , 1-20-1 Handayama, Higashi-ku, Hamamatsu, Shizuoka 431-3192, Japan.
  • Gee AD; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
  • Zhang MR; Molecular Imaging Center, National Institute of Radiological Sciences , 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
J Med Chem ; 59(12): 5847-56, 2016 06 23.
Article em En | MEDLINE | ID: mdl-27232368
ABSTRACT
Multidrug resistance-associated protein 4 (MRP4) and organic anion transporter 3 (OAT3) mediate the efflux of organic anions from the brain and heart. In this study, we have developed a probe for estimating the activity of these transporters in these tissues using positron emission tomography. Several (11)C-labeled hippuric acid ester derivatives were screened with the expectation that they would be hydrolyzed in situ to form the corresponding (11)C-labeled organic acids in target tissues. Among the compounds screened, benzyl [(11)C]hippurate showed favorable hydrolysis rates and uptake properties in the target tissues of mice. Subsequent evaluation using transporter knockout mice revealed that radioactivity was retained in the brain and heart of Oat3(-/-) and Mrp4(-/-) mice, respectively, compared with that of control mice after the intravenous administration of benzyl [(11)C]hippurate. Benzyl [(11)C]hippurate could therefore be used as a probe for estimating the activities of OAT3 and MRP4 in mouse brain and heart, respectively.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Encéfalo / Proteínas Associadas à Resistência a Múltiplos Medicamentos / Transportadores de Ânions Orgânicos Sódio-Independentes / Hipuratos Tipo de estudo: Risk_factors_studies Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Japão
Texto completo
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XML
PubMed Links
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Encéfalo / Proteínas Associadas à Resistência a Múltiplos Medicamentos / Transportadores de Ânions Orgânicos Sódio-Independentes / Hipuratos Tipo de estudo: Risk_factors_studies Limite: Animals Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2016 Tipo de documento: Article País de afiliação: Japão