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[11C]phenytoin revi...
[11C]phenytoin revisited : synthesis by [11C]CO carbonylation and first evaluation as a P-gp tracer in rats.
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Verbeek, Joost (author)
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- Eriksson, Jonas (author)
- VU University Medical Center Amsterdam
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- Syvänen, Stina (author)
- Leiden University
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Labots, Maaike (author)
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de Lange, Elizabeth C M (author)
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Voskuyl, Rob A (author)
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Mooijer, Martinus P J (author)
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Rongen, Marissa (author)
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Lammertsma, Adriaan A (author)
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Windhorst, Albert D (author)
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(creator_code:org_t)
- 2012
- 2012
- English.
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In: EJNMMI Research. - 2191-219X. ; 2:1, s. 36-
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https://doi.org/10.1...
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https://urn.kb.se/re...
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Abstract
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- ABSTRACT: BACKGROUND: At present, several positron emission tomography (PET) tracers are in use for imaging Pglycoprotein (P-gp) function in man. At baseline, substrate tracers such as R-[11C]verapamil display low brain concentrations with a distribution volume of around 1. [11C]phenytoin is supposed to be a weaker P-gp substrate, which may lead to higher brain concentrations at baseline. This could facilitate assessment of P-gp function when P-gp is upregulated. The purpose of this study was to synthesize [11C]phenytoin and to characterize its properties as a P-gp tracer. METHODS: [11C]CO was used to synthesize [11C]phenytoin by rhodium-mediated carbonylation. Metabolism and, using PET, brain pharmacokinetics of [11C]phenytoin were studied in rats. Effects of P-gp function on [11C]phenytoin uptake were assessed using predosing with tariquidar. RESULTS: [11C]phenytoin was synthesized via [11C]CO in an overall decay-corrected yield of 22 +/- 4%. At 45 min after administration, 19% and 83% of radioactivity represented intact [11C]phenytoin in the plasma and brain, respectively. Compared with baseline, tariquidar predosing resulted in a 45% increase in the cerebral distribution volume of [11C]phenytoin. CONCLUSIONS: Using [11C]CO, the radiosynthesis of [11C]phenytoin could be improved. [11C]phenytoin appeared to be a rather weak P-gp substrate.
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- By the author/editor
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Verbeek, Joost
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Eriksson, Jonas
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Syvänen, Stina
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Labots, Maaike
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de Lange, Elizab ...
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Voskuyl, Rob A
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show more...
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Mooijer, Martinu ...
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Rongen, Marissa
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Lammertsma, Adri ...
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Windhorst, Alber ...
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show less...
- Articles in the publication
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EJNMMI Research
- By the university
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Uppsala University