Sökning: id:"swepub:oai:DiVA.org:uu-185289" >
[11C]phenytoin revi...
[11C]phenytoin revisited : synthesis by [11C]CO carbonylation and first evaluation as a P-gp tracer in rats.
-
Verbeek, Joost (författare)
-
- Eriksson, Jonas (författare)
- VU University Medical Center Amsterdam
-
- Syvänen, Stina (författare)
- Leiden University
-
visa fler...
-
Labots, Maaike (författare)
-
de Lange, Elizabeth C M (författare)
-
Voskuyl, Rob A (författare)
-
Mooijer, Martinus P J (författare)
-
Rongen, Marissa (författare)
-
Lammertsma, Adriaan A (författare)
-
Windhorst, Albert D (författare)
-
visa färre...
-
(creator_code:org_t)
- 2012
- 2012
- Engelska.
-
Ingår i: EJNMMI Research. - 2191-219X. ; 2:1, s. 36-
- Relaterad länk:
-
https://doi.org/10.1...
-
visa fler...
-
https://urn.kb.se/re...
-
https://doi.org/10.1...
-
visa färre...
Abstract
Ämnesord
Stäng
- 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.
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
Hitta via bibliotek
Till lärosätets databas
- Av författaren/redakt...
-
Verbeek, Joost
-
Eriksson, Jonas
-
Syvänen, Stina
-
Labots, Maaike
-
de Lange, Elizab ...
-
Voskuyl, Rob A
-
visa fler...
-
Mooijer, Martinu ...
-
Rongen, Marissa
-
Lammertsma, Adri ...
-
Windhorst, Alber ...
-
visa färre...
- Artiklar i publikationen
-
EJNMMI Research
- Av lärosätet
-
Uppsala universitet