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Fluorine-18 isotope labeling for positron emission tomography imaging. Direct evidence for DBPR211 as a peripherally restricted CB1 inverse agonist.
Chang, Chun-Ping; Huang, Ho-Lien; Huang, Jing-Kai; Hung, Ming-Shiu; Wu, Chien-Huang; Song, Jen-Shin; Lee, Chia-Jui; Yu, Chung-Shan; Shia, Kak-Shan.
Afiliación
  • Chang CP; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC.
  • Huang HL; Department of Biomedical Engineering and Environmental Sciences, National Tsing Hua University, Hsinchu 30013, Taiwan, ROC.
  • Huang JK; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC.
  • Hung MS; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC.
  • Wu CH; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC.
  • Song JS; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC.
  • Lee CJ; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC.
  • Yu CS; Department of Biomedical Engineering and Environmental Sciences, National Tsing Hua University, Hsinchu 30013, Taiwan, ROC; Institute of Nuclear Engineering and Sciences, National Tsing Hua University, Hsinchu 30013, Taiwan, ROC. Electronic address: csyu@mx.nthu.edu.tw.
  • Shia KS; Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 35053, Taiwan, ROC. Electronic address: ksshia@nhri.org.tw.
Bioorg Med Chem ; 27(1): 216-223, 2019 01 01.
Article en En | MEDLINE | ID: mdl-30528163
The [18F] isotope-labelled CB1 inverse agonist 3 was elaborated and synthesized for positron emission tomography scanning studies. After immediate purification and calibration with its unlabeled counterpart, compound 3 was intravenously injected in mice and revealed that its distribution percentage in brain over 90-min scans among five region of interests, including brain, liver, heart, thigh muscle and kidney was lower than 1%, thus providing direct evidence to justify itself as a peripherally restricted CB1 antagonist.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Sulfonamidas / Tiofenos / Receptor Cannabinoide CB1 / Agonistas de Receptores de Cannabinoides Límite: Animals Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Sulfonamidas / Tiofenos / Receptor Cannabinoide CB1 / Agonistas de Receptores de Cannabinoides Límite: Animals Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article Pais de publicación: Reino Unido