Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species

Kiichi Ishiwata, Kazunori Kawamura, Wei Fang Wang, Hideo Tsukada, Norihiro Harada, Hideki Mochizuki, Yuichi Kimura, Kenji Ishii, Ren Iwata, Kazuhiko Yanai

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Abstract

The specific binding of [11C]doxepin, which has been used as a radioligand for mapping histamine H1 receptors in human brain by positron emission tomography, was evaluated in five animal species. In mice the [11C]doxepin uptake was reduced by treatment with cold doxepin and two H1 receptor antagonists, but not with H2/H3 antagonists. The specific binding evaluated with treatment with (+)-chlorpheniramine (H1 antagonist) was in the range of 10-30% in mouse, rat, rabbit, and monkey, but was not detected in guinea pig.

Original languageEnglish
Pages (from-to)493-502
Number of pages10
JournalNuclear Medicine and Biology
Volume31
Issue number4
DOIs
Publication statusPublished - 2004 May 1

Keywords

  • Histamine H receptor
  • Positron emission tomography
  • [C]doxepin

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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    Ishiwata, K., Kawamura, K., Wang, W. F., Tsukada, H., Harada, N., Mochizuki, H., Kimura, Y., Ishii, K., Iwata, R., & Yanai, K. (2004). Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species. Nuclear Medicine and Biology, 31(4), 493-502. https://doi.org/10.1016/j.nucmedbio.2003.11.005