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

doi:10.1016/0304-3940(92)90390-S

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

Tohoku University

Research output: Contribution to journal › Article › peer-review

58 Citations (Scopus)

Abstract

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 language	English
Pages (from-to)	145-148
Number of pages	4
Journal	Neuroscience Letters
Volume	137
Issue number	2
DOIs	https://doi.org/10.1016/0304-3940(92)90390-S
Publication status	Published - 1992 Mar 30

Keywords

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

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10.1016/0304-3940(92)90390-S

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

abstract = "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.",

keywords = "Frontal cortex, Histamine, Histamine H receptor, Human brain, In vivo study, Positron emission tomography, [C]Doxepin",

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

note = "Funding Information: The authors thank Mr. Y. Ishikawa, Mr. S. Seo, and Mr. S. Watanuki for their technical assistance. This work was supported by Grants-in-Aid from the Ministry of Education, Science and Culture (63065004, 0387027), the Ministry of Health (3-5), Terumo Life Science Foundation, and Yamanouchi Foundation for Research on Metabolic Disorders.",

year = "1992",

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day = "30",

doi = "10.1016/0304-3940(92)90390-S",

language = "English",

volume = "137",

pages = "145--148",

journal = "Neuroscience Letters",

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T1 - Histamine H1 receptors in human brain visualized in vivo by [11C]doxepin and positron emission tomography

AU - Yanai, Kazuhiko

AU - Watanabe, Takehiko

AU - Yokoyama, Hiroyuki

AU - Meguro, Kenichi

AU - Hatazawa, Jun

AU - Itoh, Masatoshi

AU - Iwata, Ren

AU - Ishiwata, Kiichi

AU - Takahashi, Toshihiro

AU - Ido, Tatsuo

N1 - Funding Information: The authors thank Mr. Y. Ishikawa, Mr. S. Seo, and Mr. S. Watanuki for their technical assistance. This work was supported by Grants-in-Aid from the Ministry of Education, Science and Culture (63065004, 0387027), the Ministry of Health (3-5), Terumo Life Science Foundation, and Yamanouchi Foundation for Research on Metabolic Disorders.

PY - 1992/3/30

Y1 - 1992/3/30

N2 - 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.

AB - 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.

KW - Frontal cortex

KW - Histamine

KW - Histamine H receptor

KW - Human brain

KW - In vivo study

KW - Positron emission tomography

KW - [C]Doxepin

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

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