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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11 Scopus citations


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 (US)
Pages (from-to)493-502
Number of pages10
JournalNuclear Medicine and Biology
Issue number4
StatePublished - May 2004
Externally publishedYes


  • 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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