TY - JOUR
T1 - Mapping of Histamine H1 Receptors in the Human Brain Using [11C]Pyrilamine and Positron Emission Tomography
AU - Yanai, Kazuhiko
AU - Watanabe, Takehiko
AU - Yokoyama, Hiroyuki
AU - Hatazawa, Jun
AU - Iwata, Ren
AU - Ishiwata, Kiichi
AU - Meguro, Kenichi
AU - Itoh, Masatoshi
AU - Takahashi, Toshihiro
AU - Ido, Tatsuo
AU - Matsuzawa, Taiju
PY - 1992/7
Y1 - 1992/7
N2 - We have studied the characteristics of carbon‐11 labeled pyrilamine as a radioligand for investigating histamine H1 receptors in human brain with positron emission tomography (PET). [11QPyrilamine is distributed evenly in proportion to cerebral blood flow at initial PET images. Later (after 45–60 min), 11C 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 H1 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 H1 receptors in vivo in humans will facilitate studies on neurological and psychiatric disorders in which histamine H1 receptors are thought to be abnormal.
AB - We have studied the characteristics of carbon‐11 labeled pyrilamine as a radioligand for investigating histamine H1 receptors in human brain with positron emission tomography (PET). [11QPyrilamine is distributed evenly in proportion to cerebral blood flow at initial PET images. Later (after 45–60 min), 11C 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 H1 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 H1 receptors in vivo in humans will facilitate studies on neurological and psychiatric disorders in which histamine H1 receptors are thought to be abnormal.
KW - Histamine
KW - Histamine H receptors
KW - Human brain
KW - In vivo study
KW - Positron emission tomography
KW - Pyrilamine
UR - http://www.scopus.com/inward/record.url?scp=0026611493&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0026611493&partnerID=8YFLogxK
U2 - 10.1111/j.1471-4159.1992.tb08883.x
DO - 10.1111/j.1471-4159.1992.tb08883.x
M3 - Article
C2 - 1613494
AN - SCOPUS:0026611493
VL - 59
SP - 128
EP - 136
JO - Journal of Neurochemistry
JF - Journal of Neurochemistry
SN - 0022-3042
IS - 1
ER -