Article Figures & Data
Figures
- FIGURE 1.
Chemical structures of 18F-THK-5105, 18F-THK-5116, 18F-THK-5117, and 18F-THK-523.
- FIGURE 2.
Radiosynthesis scheme of 18F-2-arylquinolines.
- FIGURE 3.
Competitive inhibition of 18F-THK-5105 binding by 2-arylquinolines and FDDNP to tau protein fibrils. Ki values for inhibition of 18F-THK-5105 binding to tau are shown.
- FIGURE 4.
Neuropathologic staining of brain sections from AD patients. Neurofibrillary tangles and neuropil threads were clearly stained with THK-5105 (A and C). These stainings were consistent with tau immunostaining (B) and Gallyas–Braak staining (D) in same sections. Bar = 50 μm.
- FIGURE 5.
(A) Autoradiographic images of 18F-THK-5105, 18F-THK-5117, and 11C-PiB binding in mesial temporal section from AD patient. (B) Gallyas–Braak silver staining (left) and immunostaining with anti-tau (center) and anti-Aβ (right) antibodies in adjacent brain sections. Arrowheads = CA1 area of hippocampus; longer arrows = entorhinal cortex.
- FIGURE 6.
(A) Autoradiography of hemibrain sections from AD patient with 18F-THK-5105 and tau immunostaining in neighboring section. (B) Region-of-interest analysis indicated that percentage areas of 18F-THK-5105 binding (line plots) were significantly correlated with percentage areas of tau immunostaining (gray bars) but not with that of Aβ immunostaining (white bars). CG = cingulate gyrus; HIP = hippocampus; FUG = fusiform gyrus; IHC = immunohistochemistry; INS = insula; ITG = inferior temporal gyrus; MTG = middle temporal gyrus; PCL = paracentral lobule; PHG = parahippocampal gyrus; POG = postcentral gyrus; PRG = precentral gyrus; SFG = superior frontal gyrus; STG = superior temporal gyrus.
- FIGURE 7.
Time–activity curves after intravenous administration of 18F-THK-5105 (A) and 18F-THK-5117 (B) in mice.
Tables
- TABLE 1
Log P and Brain Uptake After Intravenous Administration of 18F-Labeled Compounds in Mice
Brain uptake (%ID/g) Compound Log P 2 min after injection 30 min after injection 60 min after injection Brain uptake ratio (2 min/60 min) 18F-THK-523 2.40 2.72 1.47 1.46 1.86 18F-THK-5105 3.03 9.20 3.61 1.00 9.20 18F-THK-5116 1.57 3.36 0.75 0.57 5.89 18F-THK-5117 2.32 6.06 0.59 0.26 23.1 18F-FDDNP 3.71 6.23 2.02 2.14 2.91 Protein Kd1 Bmax1 Kd2 Bmax2 Tau 1.45 6.89 7.40 20.05 Aβ1–42 35.9 61.6 Kd are in nM and Bmax are in pmol 18F-THK-5105/nmol fibrils.
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