学術雑誌論文 [(11)C]TASP457, a novel PET ligand for histamine H3 receptors in human brain.

Kimura, Yasuyuki  ,  Seki, Chie  ,  Ikoma, Yoko  ,  Ichise, Masanori  ,  Kawamura, Kazunori  ,  Takahata, Keisuke  ,  Moriguchi, Sho  ,  Nagashima, Tomohisa  ,  Ishii, Tatsuya  ,  Kitamura, Soichiro  ,  Niwa, Fumitoshi  ,  Endo, Hironobu  ,  Yamada, Makiko  ,  Higuchi, Makoto  ,  Ming-Rong, Zhang  ,  Suhara, Tetsuya

内容記述
The histamine H3 receptors are presynaptic neuroreceptors that inhibit the release of histamine and other neurotransmitters. The receptors are considered a drug target for sleep disorders and neuropsychiatric disorders with cognitive decline. We developed a novel PET ligand for the H3 receptors, [(11)C]TASP0410457 ([(11)C]TASP457), with high affinity, selectivity and favorable kinetic properties in the monkey, and evaluated its kinetics and radiation safety profile for quantifying the H3 receptors in human brain.

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