量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum Science and Technology.
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ABSTRACT: The transmembrane α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptor regulatory protein γ-8 (TARP γ-8)
constitutes an auxiliary subunit of AMPA receptors, which mediates various
brain functions including learning and memory. TARP γ-8 has emerged as a
promising therapeutic target for central nervous system disorders. Despite
considerable efforts, previously reported TARP γ-8 PET radioligands, such as
[
11C]TARP-1903 and [11C]TARP-1811 series, were plagued by limited brain
uptake and/or high nonspecific binding in vivo. Herein, we developed two
novel 11C-labeled probes, [11C]8 and [11C]15 (also named as [11C]TARP2105), of which the latter exhibited a reasonable brain uptake as well as
specific binding toward TARP γ-8 both in vitro and in vivo, as confirmed by
blocking experiments with the commercially available TARP γ-8 inhibitor,
JNJ-55511118 in the TARP γ-8-rich hippocampus. Overall, [11C]15 exhibited
promising tracer characteristics and proved to be a lead positron-emission tomography ligand for the non-invasive quantification of
TARP γ-8 in the mammalian brain.
Imaging of transmembrane AMPA receptor regulatory protein by positron emission tomography
