[Designed molecular probes in brain research: molecular imaging of IP2 receptor in the human brain].
The study of the role of prostaglandins in living human brain requires a highly designed non-invasive molecular probe with a specific function in the central nervous system and high stability in an in vivo system in addition to the ability of blood-brain-barrier penetration. We succeeded in designing 15R-TIC, which binds with a novel prostacyclin receptor subtype (IP2) expressed specifically in the central nervous system. 15R-TIC exhibited a distinct nerve-protecting effect in both high oxygen and in vivo ischemic conditions. In addition, a rapid C-methylation reaction, developed in order to incorporate a short-lived 11C-positron nuclide into the molecule, realized the synthesis of 15R-[11C]TIC methyl ester with the radioactivity of 2.5 GBq. The molecular imaging was established for both monkey and human brains by intravenous injection of this positron emission tomography (PET) probe.
Suzuki
Masaaki
M
Division of Regeneration and Advanced Medical Science, Gifu University Graduate School of Medicine, 1-1, Yanagido, Gifu, 501-1193 Japan.
Doi
Hisashi
H
Kato
Koichi
K
Hosoya
Takamitsu
T
Watanabe
Yumiko
Y
Watanabe
Yasuyoshi
Y
D000818:Animals; D001923:Brain Chemistry; D000882:Haplorhini; D006801:Humans; D015336:Molecular Probe Techniques; D044006:Receptors, Epoprostenol / Q000032:analysis*
D044006:Receptors, Epoprostenol