Steen Jakobsen

PET neuroimaging of [11C]mirtazapine enantiomers in pigs

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Previously, we used positron emission tomography (PET) for studying the pharmacokinetics of rac-[11C]mirtazapine in living brain. Our findings showed that rac-[11C]mirtazapine has suitable properties for PET neuroimaging. However, separate studies of enantiomers are typically required for characterizing the pharmacokinetics of a racemic drug. Therefore, we have determined the whole-body distribution and brain pharmacokinetics of S- and R-[11C]mirtazapine in pigs. The enantiomers of [11C]mirtazapine produced similar effective doses of radioactivity in most body organs, except for the brain, in which the dose was approximately 40% higher after injection of S-[11C]mirtazapine than the antipode. Kinetic analyses of dynamic brain PET recordings showed that values for regional accumulation of compound (k3) were significantly higher for S-[11C]mirtazapine than for the antipode, while the values for clearance of compounds from tissue to circulation (k2) were consistently lower for S-[11C]mirtazapine than for the R-form. No reliable difference occurred in the rate of metabolism of S- and R-[11C]mirtazapine in the bloodstream of the pigs. The present findings indicate that enantioselective processes affect the cerebral pharmacokinetics of rac-mirtazapine.
Original languageEnglish
JournalEuropean Neuropsychopharmacology
Volume16
Issue5
Pages (from-to)350-7
Number of pages8
ISSN0924-977X
DOIs
Publication statusPublished - 2006

    Research areas

  • Animals, Blood Chemical Analysis, Brain, Carbon Radioisotopes, Female, Injections, Intravenous, Isotope Labeling, Mianserin, Positron-Emission Tomography, Radiometry, Radiopharmaceuticals, Stereoisomerism, Swine, Whole-Body Counting

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