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• W2189095688 abstract "Current SPECT radioligands available for in vivo imaging of the dopamine transporter (DAT) also show affinity for monoamine transporters other than DAT, especially the serotonin transporter (SERT). The effect of this lack of selectivity for in vivo imaging is unknown. In this study, we compared the SPECT radioligands 123 I-2-b-carbomethoxy-3b-(4-iodophenyl)-N-(3fluoropropyl)nortropane ( 123 I-FP-CIT) and 123 I-N-(3-iodoprop2E-enyl)-2-b-carbomethoxy-3b-(4-methylphenyl) (123I-PE2I). 123 I-FP-CIT has a 10-fold higher selectivity than 123 I-FP-CIT for DAT versus SERT. Methods: Sixteen healthy individuals were scanned in random order with both radioligands. The radioligands were administered according to standard recommendations: 123 I-FP-CIT was given as a bolus injection, and the ratio between the striatum and reference tissue was measured after 3 h. 123 I-PE2I was administered in a bolus–infusion setup, and the nondisplaceable binding potential (BPND) was measured after 2 h. To assess the contribution of SERT to the overall SPECT signal, SERT was blocked by intravenous citalopram in 6 of the individuals. Results: The striatum-to-reference ratio 2 1 of 123 I-FP-CIT was on average 18% higher than the striatal BPND of 123I-PE2I. Equal doses of radioactivity resulted in 3 times higher counting rates for 123 I-FP-CIT than for 123 I-PE2I, both in target and in reference brain regions. Citalopram infusion led to significant reductions in both striatal (22.8% 6 20.4%, P , 0.05) and thalamic (63.0% 6 47.9%, P , 0.05) 123 I-FP-CIT binding ratios, whereas BPND of 123 I-PE2I was unaltered. Likewise, blocking of SERT led to increased (21% 6 30.1%, P , 0.001) plasma 123 I-FP-CIT, probably as a result of significant blocking of peripheral SERT binding sites. By contrast, plasma 123 I-PE2I remained stable. Conclusion: 123 I-FP-CIT and 123 I-PE2I had approximately the same targetto-background ratios, but per injected megabecquerel, 123 I-FPCIT gave rise to 3-fold higher cerebral counting rates. We found that 123I-FP-CIT, but not 123I-PE2I, brain images have a highly" @default.
• W2189095688 created "2016-06-24" @default.
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• W2189095688 date "2010-01-01" @default.
• W2189095688 modified "2023-09-24" @default.
• W2189095688 title "Serotonin Transporters in Dopamine Transporter Imaging: A Head-to-Head Comparison of Dopamine Transporter" @default.
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