ArticleEJNMMI research2012
[11C]phenytoin revisited: synthesis by [11C]CO carbonylation and first evaluation as a P-gp tracer in rats.
Article in EJNMMI research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 34 citations in OpenAlex.
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- [EJNMMI radiopharmacy and chemistry · 2019Review
- Efficient synthesis of carbon-11 labelled acylsulfonamides using [Chemical communications (Cambridge, England) · 2019Article
- Chemistry for Positron Emission Tomography: Recent Advances inAngewandte Chemie (International ed. in English) · 2019Review
- Synthesis and preliminary preclinical evaluation of fluorine-18 labelled isatin-4-(4-methoxyphenyl)-3-thiosemicarbazone ([EJNMMI radiopharmacy and chemistry · 2018Article
- A [Journal of labelled compounds & radiopharmaceuticals · 2018Article
- Drug-Resistant Epilepsy: Multiple Hypotheses, Few Answers.Frontiers in neurology · 2017Review
- (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.Chemical Society reviews · 2016Review
- Advances in PET imaging of P-glycoprotein function at the blood-brain barrier.ACS chemical neuroscience · 2013Review
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10 authors at 2 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
unlabelled
backgroundAt present, several positron emission tomography (PET) tracers are in use for imaging P-glycoprotein (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.
conclusionsUsing [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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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.