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Discovery of 18F Labeled AZD5213 Derivatives as Novel Positron Emission Tomography (PET) Radioligands Targeting Histamine Subtype-3 Receptor.
Song, Zhendong; Li, Yinlong; Dahl, Kenneth; Chaudhary, Ahmad; Sun, Zhenkun; Zhou, Xin; Chen, Jiahui; Gao, Yabiao; Rong, Jian; Zhao, Chunyu; Patel, Jimmy S; Collier, Lee; Ran, Chongzhao; Zhai, Chuangyan; Zhang, Linqi; Haider, Ahmed; Mühlfenzl, Kim S; Yuan, Hongjie; Elmore, Charles S; Schou, Magnus; Liang, Steven.
Afiliación
  • Song Z; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Li Y; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Dahl K; AstraZeneca Sweden, PET Science Centre, Precision Medicine and Biosamples, SWEDEN.
  • Chaudhary A; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Sun Z; Emory University, Department of Pharmacology and Chemical Biology, UNITED STATES OF AMERICA.
  • Zhou X; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Chen J; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Gao Y; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Rong J; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Zhao C; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Patel JS; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Collier L; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Ran C; MASSACHUSETTS GENERAL HOSPITAL, Athinoula A. Martinos Center for Biomedical Imaging, UNITED STATES OF AMERICA.
  • Zhai C; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Zhang L; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Haider A; Emory University, Department of Radiology and Imaging Sciences, UNITED STATES OF AMERICA.
  • Mühlfenzl KS; AstraZeneca Gothenburg, Early Chemical Development, Pharmaceutical Sciences, SWEDEN.
  • Yuan H; Emory University, Department of Pharmacology and Chemical Biology, UNITED STATES OF AMERICA.
  • Elmore CS; AstraZeneca Gothenburg, Early Chemical Development, Pharmaceutical Sciences, SWEDEN.
  • Schou M; AstraZeneca Sweden, PET Science Centre, Precision Medicine and Biosamples, SWEDEN.
  • Liang S; Emory University, Department of Radiology and Imaging Sciences, 101 woodruff circle, Room 1206, 30322, ATLANTA, UNITED STATES OF AMERICA.
Chembiochem ; : e202400655, 2024 Sep 20.
Article en En | MEDLINE | ID: mdl-39303145
ABSTRACT
The histamine subtype 3 (H3) receptor is an important drug target in the central nervous system (CNS), and PET imaging offers a promising technique for the noninvasive evaluation of CNS disease related to the H3 receptor. In this study, we synthesized and evaluated the binding effects of [18F]H3-2404 and [18F]H3-2405 by modifying the structure of AZD5213, a selective H3 antagonist. These two radioligands were prepared in high radiochemical yields and displayed stability in serum. The in vitro autoradiographic study in rat brain tissue and the following in vivo PET studies in mice demonstrated sufficient brain uptake but predominantly non-specific distribution in rodent brain. Although these data suggest that [18F]H3-2404 and [18F]H3-2405 are unsuitable as PET tracers for brain imaging of the H3 receptor, this study provides a valuable attempt for optimizing 18F labeled radiotracers based on AZD5213.
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Estados Unidos

Texto completo: 1 Banco de datos: MEDLINE Idioma: En Revista: Chembiochem Asunto de la revista: BIOQUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Estados Unidos