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

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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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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.",

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AU - Harada, Norihiro

AU - Mochizuki, Hideki

AU - Kimura, Yuichi

AU - Ishii, Kenji

AU - Iwata, Ren

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