Histamine H1 receptors in human brain visualized in vivo by [11C]doxepin and positron emission tomography

Kazuhiko Yanai, Takehiko Watanabe, Hiroyuki Yokoyama, Kenichi Meguro, Jun Hatazawa, Masatoshi Itoh, Ren Iwata, Kiichi Ishiwata, Toshihiro Takahashi, Tatsuo Ido

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57 Citations (Scopus)


Histamine H1 receptors in the living human brain were visualized by positron emission tomography (PET) using [N-11C-methyl]-(E)-doxepin([11C]doxepin). The regional distribution of the carbon-11-labeled compound in the brain corresponded well with that of the histamine H1 receptors measured in vitro using [3H]pyrilamine. The radioactivity in the brain was significantly reduced by intravenous pretreatment with d-chlorpheniramine (5 mg). a histamine H1 antagonist. The regional distribution of [11C]doxepin in the brain 45-90 min after its injection was almost the same as that of [11C]pyrilamine in the brain. These results indicate that [11C]doxepin is useful for measuring histamine H1 receptors in human brain by PET.

Original languageEnglish
Pages (from-to)145-148
Number of pages4
JournalNeuroscience Letters
Issue number2
Publication statusPublished - 1992 Mar 30


  • Frontal cortex
  • Histamine
  • Histamine H receptor
  • Human brain
  • In vivo study
  • Positron emission tomography
  • [C]Doxepin

ASJC Scopus subject areas

  • Neuroscience(all)


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