Your browser doesn't support javascript.
loading
[11C]NCGG401, a novel PET ligand for imaging of colony stimulating factor 1 receptors.
Ogata, Aya; Ji, Bin; Yamada, Takashi; Hattori, Saori; Abe, Junichiro; Ikenuma, Hiroshi; Ichise, Masanori; Koyama, Hiroko; Suzuki, Masaaki; Kato, Takashi; Ito, Kengo; Kimura, Yasuyuki.
Affiliation
  • Ogata A; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan; Department of Pharmacy, Faculty of Pharmacy, Gifu University of Medical Science (GUMS), Kani, Japan. Electronic address:
  • Ji B; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan; Department of Functional Brain Imaging Research, National Institute of Radiological Sciences, National Institutes for Qua
  • Yamada T; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Hattori S; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Abe J; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Ikenuma H; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Ichise M; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan; Department of Functional Brain Imaging Research, National Institute of Radiological Sciences, National Institutes for Qua
  • Koyama H; Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University, Gifu, Japan.
  • Suzuki M; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Kato T; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Ito K; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan.
  • Kimura Y; Department of Clinical and Experimental Neuroimaging, Center for Development of Advanced Medicine for Dementia, National Center for Geriatrics and Gerontology (NCGG), Obu, Japan; Department of Functional Brain Imaging Research, National Institute of Radiological Sciences, National Institutes for Qua
Bioorg Med Chem Lett ; 65: 128704, 2022 06 01.
Article in En | MEDLINE | ID: mdl-35351586
ABSTRACT
Colony-stimulating factor 1 receptors (CSF1R) are expressed exclusively on microglia in the central nervous system. The receptors regulate immune responses by controlling the survival and activity of microglia and are intricately involved in the pathophysiology of Alzheimer's disease. In this study, we developed [11C]NCGG401, a positron emission tomography (PET) ligand, targeting for CSF1R as an imaging biomarker for microglial pathophysiology in Alzheimer's disease. NCGG401 showed a high potency to inhibit human CSF1R kinase activity and a high binding affinity to human CSF1R. PET imaging with [11C]NCGG401 in healthy rats showed a good brain permeability. Furthermore, the specific binding component was determined by postmortem autoradiography in rat brain and human hippocampal sections. The knowledge of the characteristics of [11C]NCCC401, our initial CSF1R compound, we have obtained may be useful for further development and optimization of CSF1R radioligands for PET imaging of microglia.
Subject(s)
Key words
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Macrophage Colony-Stimulating Factor / Alzheimer Disease Type of study: Prognostic_studies Limits: Animals Language: En Year: 2022 Type: Article
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Macrophage Colony-Stimulating Factor / Alzheimer Disease Type of study: Prognostic_studies Limits: Animals Language: En Year: 2022 Type: Article