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Mapping of Histamine H 1 Receptors in the Human Brain Using [ 11 C]Pyrilamine and Positron Emission Tomography
Author(s) -
Yanai Kazuhiko,
Watanabe Takehiko,
Yokoyama Hiroyuki,
Hatazawa Jun,
Iwata Ren,
Ishiwata Kiichi,
Meguro Kenichi,
Itoh Masatoshi,
Takahashi Toshihiro,
Ido Tatsuo,
Matsuzawa Taiju
Publication year - 1992
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1992.tb08883.x
Subject(s) - cerebellum , histamine , histamine h3 receptor , histamine h1 receptor , radioligand , thalamus , histamine receptor , temporal cortex , pyrilamine , receptor , hippocampus , cortex (anatomy) , positron emission tomography , in vivo , cerebral cortex , chemistry , medicine , endocrinology , neuroscience , biology , antagonist , microbiology and biotechnology
We have studied the characteristics of carbon‐11 labeled pyrilamine as a radioligand for investigating histamine H 1 receptors in human brain with positron emission tomography (PET). [ 11 QPyrilamine is distributed evenly in proportion to cerebral blood flow at initial PET images. Later (after 45–60 min), 11 C radioactivity was observed at high concentrations in the frontal and temporal cortex, hippocampus, and thalamus, and at low concentrations in the cerebellum and pons. The regional distribution of the carbon‐11 labeled compound in the brain corresponded well with that of the histamine H 1 receptors determined in vitro in autopsied materials. In six controls, the frontal and temporal cortices/cerebellum ratio increased during the first 60 min to reach a value of 1.22 ± 0.071. Intravenous administration of d ‐chlorpheniramine (5 mg) completely abolished the specific binding in vivo in the frontal cortex and temporal cortex (cortex/cerebellum ratio, 0.955 ±0.015). The availability of this method for measuring histamine H 1 receptors in vivo in humans will facilitate studies on neurological and psychiatric disorders in which histamine H 1 receptors are thought to be abnormal.