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

doi:10.1016/j.nucmedbio.2003.11.005

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

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

11 Scopus citations

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 language	English (US)
Pages (from-to)	493-502
Number of pages	10
Journal	Nuclear Medicine and Biology
Volume	31
Issue number	4
DOIs	https://doi.org/10.1016/j.nucmedbio.2003.11.005
State	Published - May 2004
Externally published	Yes

Keywords

Histamine H receptor
Positron emission tomography
[C]doxepin

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.nucmedbio.2003.11.005

Cite this

Evaluation of in vivo selective binding of [¹¹C]doxepin to histamine H₁ receptors in five animal species. / Ishiwata, Kiichi; Kawamura, Kazunori; Wang, Wei Fang; Tsukada, Hideo; Harada, Norihiro; Mochizuki, Hideki; Kimura, Yuichi; Ishii, Kenji; Iwata, Ren; Yanai, Kazuhiko.

In: Nuclear Medicine and Biology, Vol. 31, No. 4, 05.2004, p. 493-502.

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

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

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.",

keywords = "Histamine H receptor, Positron emission tomography, [C]doxepin",

author = "Kiichi Ishiwata and Kazunori Kawamura and Wang, {Wei Fang} and Hideo Tsukada and Norihiro Harada and Hideki Mochizuki and Yuichi Kimura and Kenji Ishii and Ren Iwata and Kazuhiko Yanai",

note = "Funding Information: This work was supported in part by Grants-in-Aid for Scientific Research from the Ministry of Education, Science, Sports and Culture, Japan, and for Creative Scientific Research of Japan Society for the Promotion of Science.",

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AU - Ishiwata, Kiichi

AU - Kawamura, Kazunori

AU - Wang, Wei Fang

AU - Tsukada, Hideo

AU - Harada, Norihiro

AU - Mochizuki, Hideki

AU - Kimura, Yuichi

AU - Ishii, Kenji

AU - Iwata, Ren

AU - Yanai, Kazuhiko

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AB - 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.

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KW - Positron emission tomography

KW - [C]doxepin

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