Article Figures & Data
Figures
- FIGURE 1.
Attempted radiosynthesis of carrier-added DuP-697 (compound 1) via 18F for 19F exchange reaction, which resulted in formation of 18F-desbromo-DuP-697 (compound 2). DMSO = dimethyl sulfoxide.
- FIGURE 2.
Preparation of radiopharmaceutical precursor (compound 4) from compound 3 (18), followed by labeling of noncarrier-added 18F-desbromo-DuP-697 (compound 18F-2). mCPBA = 3-chloroperbenzoic acid; DMF = N,N-dimethylformamide.
- FIGURE 3.
Phosphor images of 18F-desbromo-DuP-697 binding in coronal 80-μm-thick brain slices of untreated (top row) and NS-398 pretreated (bottom row) rats, which were killed 120 min after administration of 19 MBq of radioligand.
- FIGURE 4.
COX peroxidase activity in rat tissue, as assayed by COX-catalyzed oxidation of TMPD with hydrogen peroxide (n = 4).
Tables
- TABLE 1
Tissue Distribution of 18F-Desbromo-DuP-697 in Rats 120 Minutes After Tracer Injection
Tissue Control NS-398 (1.5 mg/kg) Indomethacin (1.5 mg/kg) Blood cells 0.08 ± 0.00 0.06 ± 0.01* 0.03 ± 0.01† Bone 0.09 ± 0.02 0.10 ± 0.03 0.07 ± 0.01 Cerebellum 0.18 ± 0.01 0.10 ± 0.01† 0.11 ± 0.03* Cerebrum 0.18 ± 0.03 0.11 ± 0.01* 0.11 ± 0.03‡ Colon 0.21 ± 0.04 0.14 ± 0.05 0.14 ± 0.05 Duodenum 2.41 ± 2.45 2.63 ± 0.62 1.01 ± 0.71 Fat 1.69 ± 0.67 1.62 ± 0.92 1.03 ± 0.57 Heart 0.34 ± 0.15 0.14 ± 0.01‡ 0.13 ± 0.03‡ Ileum 3.03 ± 4.70 2.07 ± 1.83 1.52 ± 2.32 Kidney 0.51 ± 0.11 0.28 ± 0.03* 0.25 ± 0.05* Liver 0.55 ± 0.30 0.40 ± 0.07 0.38 ± 0.09 Lung 0.66 ± 0.47 0.19 ± 0.02 0.17 ± 0.04 Muscle 0.19 ± 0.07 0.13 ± 0.03 0.14 ± 0.05 Pancreas 0.51 ± 0.10 0.41 ± 0.06 0.38 ± 0.25 Paw, control 0.20 ± 0.06 0.17 ± 0.02 0.17 ± 0.07 Paw, inflamed 0.17 ± 0.04 0.15 ± 0.02 0.14 ± 0.04 Spleen 0.10 ± 0.02 0.07 ± 0.01 0.07 ± 0.02‡ Tissue uptake is expressed as SUV ± SD (n = 4). Values were analyzed using Student’s t test with P as dual-tail probability. Significant differences between experimental groups, pretreated with either selective COX-2 inhibitor NS-398 or nonselective inhibitor indomethacin, and control group are indicated with symbols
↵* P < 0.01,
↵† P < 0.0001, and
↵‡ P < 0.05.
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