Histamine H1 receptors in human brain visualized in vivo by [11C]doxepin and positron emission tomography.
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.
Yanai
K
K
Department of Pharmacology I, School of Medicine, Tohoku University, Sendai, Japan.
Watanabe
T
T
Yokoyama
H
H
Meguro
K
K
Hatazawa
J
J
Itoh
M
M
Iwata
R
R
Ishiwata
K
K
Takahashi
T
T
Ido
T
T
D000328:Adult; D001921:Brain / Q000033:anatomy & histology / Q000378:metabolism*; D002247:Carbon Isotopes; D002744:Chlorpheniramine / Q000494:pharmacology; D004316:Doxepin; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D011738:Pyrilamine / Q000493:pharmacokinetics; D011969:Receptors, Histamine H1 / Q000378:metabolism*; D014055:Tomography, Emission-Computed
D002247:Carbon Isotopes; D011969:Receptors, Histamine H1; D004316:Doxepin; D002744:Chlorpheniramine; D011738:Pyrilamine