PET evaluation of a tetracyclic, atypical antidepressant, [N-methyl-11C]mianserin, in the living porcine brain

Nuclear Medicine and Biology
Katalin MarthiD F Smith

Abstract

We synthesized [N-methyl-11C]mianserin by alkylation of N-desmethyl mianserin with [11C]methyl iodide followed by HPLC purification. We used PET for determining the regional cerebral pharmacokinetics of the radiotracer in anesthetized swine. [N-methyl-11C]Mianserin entered most brain regions readily (range of K1 values: 0.66-1.13), reaching highest levels in the basal ganglia and thalamus. The binding potential of [N-methyl-11C]mianserin was relatively low (range: 0.07-0.50), but regional differences were nonetheless observed, with highest values in the temporal cortex and lowest values in the brainstem. These PET findings, which are the first ones for a tetracyclic, antidepressant drug, show that [N-methyl-11C]mianserin has only a limited degree of regional specificity of binding in the living brain.

References

Jul 1, 1968·The Journal of Comparative Neurology·J E Breazile, R L Kitchell
Jan 1, 1983·Acta Psychiatrica Scandinavica. Supplementum·R M Pinder, A M van Delft
Jan 1, 1983·British Journal of Clinical Pharmacology·R M Pinder, A M Van Delft
Jul 28, 1999·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·D F SmithA Gjedde
Aug 17, 1999·The British Journal of Psychiatry : the Journal of Mental Science·M PoyurovskyA Weizman
Jan 7, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·D F Smith

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Citations

Sep 5, 2002·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Katalin MarthiDonald F Smith
Mar 7, 2006·Bioorganic & Medicinal Chemistry·M Van der MeyJ E Leysen
Jul 27, 2007·Psychopharmacology·Donald F SmithRaben Rosenberg
Feb 3, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Anna KrzyczmonikOlof Solin
Sep 10, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Santosh Reddy AlluriKun-Eek Kil
May 13, 2021·The World Journal of Biological Psychiatry : the Official Journal of the World Federation of Societies of Biological Psychiatry·C B EapC Hiemke

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