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Figure 1.

Structure of 1 (BAY 85-8050), 2 ([18F](2S, 4R)4F-GLN), 3 (BAY 94-9392), and 4 ([18F]FPMET).

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Figure 2.

Scheme of the radiosynthesis of [18F]FPGLU.

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Figure 3.

HPLC chromatograms of [18F]FPGLU and cold FPGLU.

(Two peaks represent a mixture containing two epimers of [18F]FPGLU or FPGLU.).

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Figure 4.

Scheme of the radiosynthesis of [11C]MGLU.

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Figure 5.

PET images of Kunming mouse with S180 fibrosarcoma.

Images obtained with either [18F]FPGLU, [18F]FPGLU ester, or [11C]MGLU at 1 h after intravenous injection. Images are shown in both transaxial and coronal slices. (The red arrows indicate tumor.).

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Figure 6.

Uptake of [18F]FPGLU in SPCA-1 cells in presence of inhibitors for systems L, A, ASC, XC, and XAG in the medium of presence and absence of Na+.

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Table 1.

Biodistribution of [18F]FPGLU in Normal Micea.

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Figure 7.

Small animal PET imaging and quantification.

Decay-corrected whole-body PET images were acquired at different time points. (A) PET images of S180 fibrosarcoma-bearing mouse static scans at 0.5, 1, 1.5, and 2 h after the injection of [18F]FPGLU. The same S180 fibrosarcoma-bearing mouse static scan at 1 h after injection of [18F]FDG. (The red arrows indicate the tumor.) (B) PET images of SPCA-1 or LTEP-a-2 human lung adenocarcinoma-bearing nude mouse static scans at 1 h after the injection of [18F]FPGLU or [18F]FDG. (The red arrows indicate the tumor.) (C) A comparison of tumor uptake of [18F]FPGLU and [18F]FDG in S180 fibrosarcoma, LTEP-a-2, and SPCA-1 human lung adenocarcinoma at 1 h after injection. (n = 3 per group; bars represent means ± SD.).

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Figure 8.

Radio-HPLC analysis the stability of [18F]FPGLU.

HPLC chromatograms of tumor tissue extract (A) and plasma (B) (S180 fibrosarcoma-bearing mice at 0.5 h after intravenous injection of [18F]FPGLU). HPLC chromatograms of urine (C) (S180 fibrosarcoma-bearing mice at 1 h after intravenous injection of [18F]FPGLU). HPLC chromatograms of [18F]FPGLU in mouse serum at 37°C for 2 h (D). (The peak at T = 5.5 min was [18F]FPGLU.).

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