(90)Y-edotreotide treatment improved symptoms associated with malignant carcinoid among subjects with no treatment alternatives. Treatment was well-tolerated and had an acceptable expected AE profile.
The uptake of MIBG, a scintigraphic agent widely used in the detection of APUD tumours, was studied with a pharmacological approach on an in vitro and an in vivo models. MIBG as well as norepinephrine (NE) was taken up by human blood platelets, a model for presynaptic nerve endings amine uptake, with a thermodependant mechanism. MIBG and NE uptake was inhibited by desimipramine and reserpine. However, MIBG but not NE uptake was inhibited by fluvoxamine, a serotonin (5HT) uptake inhibitor. This suggests that MIBG is a NE and also a 5HT uptake tracer which involves uptake one and vesicular storage mechanisms. In rats treated with 6-hydroxydopamine to induce a chemical sympathectomy, we observed an inhibition of uptake similar for MIBG and NE in the heart, the salivary glands and the spleen, but no effect was observed in the liver. Some clinical inferences to best investigate specific monoamine uptake are drawn from these results.
The iodine-123 labelled selective ligand N-(3-iodoprop-2E-enyl)-2-beta-carbomethoxy-3beta-(4-methylphenyl) nortropane ([123I]PE2I) was evaluated as a probe for in vivo dopamine transporter imaging in the human brain. Six healthy subjects were imaged with a high-resolution single-photon emission tomography scanner. Striatal radioactivity peaked at 1 h after injection. The background radioactivity was low. The volume of distribution in the striatum was 94+/-24 ml/ml. The results were compared with those of [123I]beta-CIT imaging. There was no significant uptake of [123I]PE2I in serotonin-rich regions such as the midbrain, hypothalamus and anterior gingulus, suggesting that in vivo binding is specific for the dopamine transporter. One main polar metabolite of [123I]PE2I was found in plasma, and the parent plasma concentration decayed rapidly. Radiation exposure to the study subject is 0.022+/-0.004 mSv/MBq (effective dose). The preliminary results suggest that [123I]PE2I is a selective SPET ligand for imaging striatal dopamine transporter density.
This study was designed to select a suitable solid bolus for esophageal scintigraphy. Optimally, a bolus should leave minimal residual buccal and pharyngeal activity after being swallowed. We compared the oropharyngeal behavior of three boluses, i.e., omelette, egg white, and paté of 1- and 3-ml volume. Thirty patients without dysfunction of the upper esophageal sphincter were recruited for the study. Scintigraphy interpretation was based on the results of condensed images and time activity curves. A total of 108 oropharyngeal transits were analyzed. First we determined the most appropriate volume (1 or 3 ml) of paté, omelette, and egg white (i.e., the volume with the least residual oropharyngeal activity). Buccal or pharyngeal bolus retention occurred significantly less frequently with 1 ml paté than 3 ml (p = 0.03) and also less frequently with 3 ml egg white than with 1 ml egg white (p = 0.03), and the mean buccal bolus retention index was lower using 3 ml omelette than 1 ml omelette (p = 0.03). Then we identified the most suitable of the three selected boluses. Both oral and pharyngeal residues were higher for paté (1 ml) than for omelette (p = 0.02 and 0.05), and pharyngeal residue was significantly lower for omelette (3 ml) than for egg white (3 ml) (p = 0.02). In conclusion, a 3-ml bolus of radiolabeled omelette seems to be the most suitable bolus for exploration of esophageal transit, and its use could enhance the potential of scintigraphy in the assessment of esophageal disorders.
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