Document Detail


PET neuroimaging of [11C]mirtazapine enantiomers in pigs.
MedLine Citation:
PMID:  16361085     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Donald F Smith; Katalin Marthi; Ole L Munk; Paul Cumming; Søren B Hansen; Steen Jakobsen
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2005-12-19
Journal Detail:
Title:  European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology     Volume:  16     ISSN:  0924-977X     ISO Abbreviation:  Eur Neuropsychopharmacol     Publication Date:  2006 Jul 
Date Detail:
Created Date:  2006-06-06     Completed Date:  2006-08-18     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9111390     Medline TA:  Eur Neuropsychopharmacol     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  350-7     Citation Subset:  IM    
Affiliation:
Center for Basic Psychiatric Research, Psychiatric Hospital of Aarhus University, 8240 Risskov, Denmark. dfsmith@inet.uni2.dk
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MeSH Terms
Descriptor/Qualifier:
Animals
Blood Chemical Analysis
Brain / radionuclide imaging
Carbon Radioisotopes / diagnostic use
Female
Injections, Intravenous
Isotope Labeling
Mianserin / analogs & derivatives*,  blood,  pharmacokinetics
Positron-Emission Tomography
Radiometry
Radiopharmaceuticals / blood,  pharmacokinetics*
Stereoisomerism
Swine
Whole-Body Counting
Chemical
Reg. No./Substance:
0/Carbon Radioisotopes; 0/Radiopharmaceuticals; 24219-97-4/Mianserin; 61337-67-5/mirtazapine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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