title: Trifluoromethoxy-benzylated ligands improve amyloid detection in the brain using (19)F magnetic resonance imaging.
abstract: The chemical properties of probes that improve amyloid detection by non-invasive (19)F magnetic resonance imaging (MRI) are of interest. We synthesized benzoxazole compounds with trifluoromethoxy groups, and found that these compounds displayed sharp (19)F nuclear magnetic resonance (NMR) signals in an assay buffer. However, the intensities of the (19)F NMR signals were dramatically reduced in mouse brain lysates. Our results indicate that the inhibitory effect of brain tissue on the (19)F NMR signals from these probes can be attributed to the hydrophobicity of the tissue. These results highlight the importance of using hydrophilic (19)F-MRI agents to avoid the inhibitory effects of brain tissues on (19)F NMR signals.
authors.affiliation: Molecular Neuroscience Research Center, Shiga University of Medical Science, Setatsukinowa-cho, Otsu 520-2192, Japan.
authors.forename: Tomone
authors.initials: T
authors.lastname: Amatsubo
authors.forename: Shigehiro
authors.initials: S
authors.lastname: Morikawa
authors.forename: Toshio
authors.initials: T
authors.lastname: Inubushi
authors.forename: Makoto
authors.initials: M
authors.lastname: Urushitani
authors.forename: Hiroyasu
authors.initials: H
authors.lastname: Taguchi
authors.forename: Nobuaki
authors.initials: N
authors.lastname: Shirai
authors.forename: Koichi
authors.initials: K
authors.lastname: Hirao
authors.forename: Masanari
authors.initials: M
authors.lastname: Kato
authors.forename: Kyuya
authors.initials: K
authors.lastname: Morino
authors.forename: Hirohiko
authors.initials: H
authors.lastname: Kimura
authors.forename: Ichiro
authors.initials: I
authors.lastname: Nakano
authors.forename: Chikako
authors.initials: C
authors.lastname: Yoshida
authors.forename: Takashi
authors.initials: T
authors.lastname: Okada
authors.forename: Mitsuo
authors.initials: M
authors.lastname: Sano
authors.forename: Ikuo
authors.initials: I
authors.lastname: Tooyama
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis* / Q000378:metabolism / Q000503:physiopathology; D000682:Amyloid / Q000032:analysis*; D000818:Animals; D001583:Benzoxazoles / Q000737:chemistry / Q000493:pharmacokinetics; D001812:Blood-Brain Barrier / Q000187:drug effects / Q000378:metabolism; D001921:Brain / Q000378:metabolism / Q000473:pathology* / Q000503:physiopathology; D017611:Fluorine Compounds / Q000737:chemistry / Q000493:pharmacokinetics; D008024:Ligands; D008279:Magnetic Resonance Imaging / Q000379:methods*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D058225:Plaque, Amyloid / Q000378:metabolism / Q000473:pathology*
chemical_list: D000682:Amyloid; D001583:Benzoxazoles; D017611:Fluorine Compounds; D008024:Ligands