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

K Yanai, T Watanabe, H Yokoyama, K Meguro, J Hatazawa, M Itoh, R Iwata, K Ishiwata, T Takahashi, T Ido
Neuroscience Letters 1992 March 30, 137 (2): 145-8
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.

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