Article Figures & Data
Figures
- FIGURE 1.
Chemical structure of the 99mTc(N)-compounds, with their corresponding physical properties.
- FIGURE 2.
HPLC profiles of 99mTc(N)-DBODC(3/5) incubated at 37°C for 60 min in human serum. HS = ultraviolet trace of human serum detected at 215 nm (albumin tr = 14.42 min); 99mTc(N)-DBODC(3) tr = 18.9 min; 99mTc(N)-DBODC(5) tr = 19.76 min. Superimposable HPLC profiles were obtained at 2 min. Similar results were observed in rat serum.
- FIGURE 3.
Time–activity curves of liver (A), kidneys (B), intestinal tissue (C), and endoluminal content (D) before (baseline) and after cyclosporin A administration for female, baseline (•); female, cyclosporin A (▪); male, baseline (○); and male, cyclosporin A (□).
- FIGURE 4.
HPLC profiles of 99mTc(N)-DBODC(5) complexes after tissue extraction at 120 min after injection. Peaks represent control (A); activity extracted from myocardial tissue after treatment with saline (B) or treatment with MeCN (C); and activity extracted with MeCN from liver (D), endoluminal content (E), kidneys (F), and directly from urine (G) of male rats. No hepatic biotransformation of tracers was observed at 30 min after injection. No changes in tracer identity were found in tissues and fluids of female rats at 30 and 120 min after injection. Similar results were observed for 99mTc(N)-DBODC(3).
- FIGURE 5.
(A) Percentage of distribution of 99mTc-activity in fractions obtained from isolated rat hearts, with values expressed as percentage of total recoverable activity. (B) Percentage of distribution of malate dehydrogenase activity in each tissue fraction. (C) Correlative 99mTc-activity and malate dehydrogenase content in “cytosolic” fractions.
- FIGURE 6.
(A) Effects of CCCP (5 μM) on 99mTc-activity content in each fraction. (B) CCCP-releasable 99mTc-activity in fragment and mitochondrial fraction.
- FIGURE 7.
Corrected fractional subcellular distribution of 99mTc-activity expressed as percentage of total activity. 99mTc-activity associated with malate dehydrogenase in supernatants I and II, or releasable by treatment of pellets with CCCP, was assigned to mitochondrial fraction. CCCP-insensitive 99mTc-activity in nonmitochondrial pellet was assigned to fragments, and all residual activity was assigned to cytosol.
Tables
% dose/g for 3 rats (mean ± SD) Group* Organ 2 min 10 min 30 min 60 min 120 min A Blood 0.13 ± 0.04 0.03 ± 0.02 0.02 ± 0.00 0.02 ± 0.01 0.01 ± 0.00 Heart 2.85 ± 0.09 2.82 ± 0.05 3.01 ± 0.30 2.98 ± 0.04 2.82 ± 0.04 Lungs 1.18 ± 0.06 0.63 ± 0.04 0.55 ± 0.02 0.59 ± 0.01 0.34 ± 0.02 Liver 1.53 ± 0.29 0.43 ± 0.12 0.18 ± 0.02 0.10 ± 0.01 0.06 ± 0.01 Kidneys 8.54 ± 0.12 7.32 ± 0.09 4.86 ± 0.04 4.05 ± 0.06 2.87 ± 0.02 Small intestine 11.01 ± 0.52 15.21 ± 1.94 6.22 ± 0.39 7.45 ± 0.12 15.51 ± 0.29 Muscle 0.21 ± 0.02 0.25 ± 0.04 0.26 ± 0.03 0.32 ± 0.02 0.38 ± 0.03 Urine — — 7.41 ± 0.53 — 20.51 ± 0.56 Heart-to-lung ratio 2.41 4.47 5.47 5.05 8.35 Heart-to-liver ratio 1.86 6.55 16.72 29.80 47.00 B Blood 0.14 ± 0.05 0.03 ± 0.01 0.02 ± 0.00 0.02 ± 0.01 0.01 ± 0.00 Heart 2.95 ± 0.09 2.84 ± 0.05 3.02 ± 0.30 2.91 ± 0.04 2.75 ± 0.04 Lungs 0.88 ± 0.06 0.64 ± 0.05 0.57 ± 0.02 0.39 ± 0.01 0.29 ± 0.02 Liver 2.53 ± 0.25 1.43 ± 0.12 0.64 ± 0.02 0.20 ± 0.01 0.11 ± 0.01 Kidneys 14.12 ± 1.25 10.12 ± 1.51 6.70 ± 0.98 5.98 ± 0.68 3.32 ± 0.21 Small intestine 5.97 ± 2.52 9.59 ± 1.02 6.22 ± 0.50 6.57 ± 1.39 6.91 ± 2.39 Muscle 0.23 ± 0.03 0.21 ± 0.01 0.18 ± 0.02 0.15 ± 0.01 0.16 ± 0.05 Urine — — 0.57 ± 0.09 — 16.61 ± 1.40 Heart-to-lung ratio 3.35 4.44 5.29 7.46 9.48 Heart-to-liver ratio 1.16 1.98 4.71 14.55 25.00 C Blood 0.31 ± 0.03 0.15 ± 0.01 0.12 ± 0.02 0.06 ± 0.00 0.15 ± 0.01 Heart 3.09 ± 0.22 3.17 ± 0.30 3.00 ± 0.21 2.99 ± 0.03 2.72 ± 0.19 Lungs 1.83 ± 0.02 1.16 ± 0.07 0.74 ± 0.02 0.56 ± 0.23 0.62 ± 0.06 Liver 2.21 ± 0.03 1.43 ± 0.30 0.88 ± 0.08 0.53 ± 0.04 0.63 ± 0.09 Kidneys 14.91 ± 1.20 11.59 ± 0.98 7.83 ± 0.13 6.87 ± 0.05 5.69 ± 1.25 Small intestine 1.51 ± 0.17 8.05 ± 1.21 8.96 ± 1.75 11.21 ± 0.87 12.14 ± 4.17 Muscle 0.30 ± 0.03 0.30 ± 0.04 0.36 ± 0.08 0.30 ± 0.10 0.38 ± 0.05 Urine — 14.35 ± 4.18 12.78 ± 4.22 — 16.51 ± 1.44 Heart-to-lung ratio 1.69 2.74 4.04 5.39 4.38 Heart-to-liver ratio 1.40 2.22 3.39 5.69 4.30 ↵* A = 99mTc(N)-DBODC(3) in female rats; B = 99mTc(N)-DBODC(5) in female rats; C = 99mTc(N)-DBODC(5) in male rats.
- TABLE 2
Sex-Related Effects of Cyclosporine A on Biodistribution Profile of 99mTc(N)-DBODC(5)
% dose/g for 3 rats (mean ± SD) Female (baseline) Female (cyclosporin A) Male (baseline) Male (cyclosporin A) Organ 30 min 120 min 30 min 120 min 30 min 120 min 30 min 120 min Blood 0.02 ± 0.00 0.01 ± 0.00 0.03 ± 0.01 0.01 ± 0.00 0.12 ± 0.02 0.15 ± 0.01 0.12 ± 0.03 0.05 ± 0.01 Heart 3.02 ± 0.30 2.75 ± 0.04 3.51 ± 0.19 3.50 ± 0.20 3.00 ± 0.21 2.72 ± 0.19 3.71 ± 0.51 3.51 ± 0.09 Lungs 0.57 ± 0.13 0.29 ± 0.02 0.91 ± 0.05 0.54 ± 0.03 0.74 ± 0.02 0.62 ± 0.06 1.64 ± 0.41 0.76 ± 0.16 Liver 0.64 ± 0.02 0.11 ± 0.01 0.72 ± 0.06 0.69 ± 0.11 0.88 ± 0.08 0.63 ± 0.09 2.83 ± 0.10 1.80 ± 0.60 Kidneys 6.70 ± 0.98 3.32 ± 0.21 8.21 ± 0.98 9.57 ± 0.89 7.83 ± 0.13 5.69 ± 1.25 13.82 ± 1.00 12.96 ± 2.46 Small intestine 6.22 ± 0.50 6.91 ± 2.39 9.78 ± 0.58 15.08 ± 2.09 8.96 ± 1.75 12.14 ± 4.17 10.65 ± 1.32 8.02 ± 1.63 Intestinal tissue* 7.80 ± 0.39 8.92 ± 2.00 59.86 ± 10.39 44.65 ± 1.48 66.33 ± 0.65 61.51 ± 9.21 63.64 ± 10.90 28.18 ± 4.57 Endoluminal* 92.00 ± 0.39 90.05 ± 2.00 40.14 ± 10.39 55.35 ± 1.48 33.67 ± 0.65 38.49 ± 9.21 36.36 ± 10.90 71.82 ± 4.57 Urine 0.57 ± 0.09 16.61 ± 1.40 8.94 ± 0.29 8.27 ± 3.40 12.78 ± 4.22 14.82 ± 1.44 NA 16.91 ± 2.59 Heart-to-lung ratio 5.29 9.48 3.85 6.48 4.04 4.38 2.26 4.62 Heart-to-liver ratio 4.71 25.00 4.87 5.07 3.39 4.30 1.31 1.95 ↵* As relative percentage of total small-intestinal activity.
NA = data not available.
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