Research
Print page Print page
Switch language
Rigshospitalet - a part of Copenhagen University Hospital
Published

Direct comparison of [(18) F]MH.MZ and [(18) F]altanserin for 5-HT(2A) receptor imaging with PET

Research output: Contribution to journalJournal articleResearchpeer-review

DOI

  1. Similar serotonin-2A receptor binding in rats with different coping styles or levels of aggression

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Acute social defeat does not alter cerebral 5-HT2A receptor binding in male Wistar rats

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Transient activation of mTOR following forced treadmill exercise in rats

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human

    Research output: Contribution to journalJournal articleResearchpeer-review

  1. A Single Dose of Psilocybin Increases Synaptic Density and Decreases 5-HT2A Receptor Density in the Pig Brain

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Effects of a single dose of psilocybin on behaviour, brain 5-HT2A receptor occupancy and gene expression in the pig

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Plasma psilocin critically determines behavioral and neurobiological effects of psilocybin

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Imaging of the Serotonin System: Radiotracers and Applications in Memory Disorders

    Research output: Chapter in Book/Report/Conference proceedingBook chapterEducation

  5. Metaboliske, endokrine og andre systemiske sygdomme

    Research output: Chapter in Book/Report/Conference proceedingBook chapterEducation

View graph of relations
Imaging the cerebral serotonin 2A (5-HT(2A) ) receptors with positron emission tomography (PET) has been carried out in humans with [(11) C]MDL 100907 and [(18) F]altanserin. Recently, the MDL 100907 analogue [(18) F]MH.MZ was developed combining the selectivity profile of MDL 100907 and the favourable radiophysical properties of fluorine-18. Here, we present a direct comparison of [(18) F]altanserin and [(18) F]MH.MZ. 5-HT(2A) receptor binding in pig cortex and cerebellum was investigated by autoradiography with [(3) H]MDL 100907, [(18) F]MH.MZ, and [(18) F]altanserin. [(18) F]MH.MZ and [(18) F]altanserin were investigated in Danish Landrace pigs by brain PET scanning at baseline and after i.v. administration of blocking doses of ketanserin. Full arterial input function and HPLC analysis allowed for tissue-compartment kinetic modelling of PET data. In vitro autoradiography showed high binding in cortical regions with both [(18) F]MH.MZ and [(18) F]altanserin. Significant 5-HT(2A) receptor binding was also found in the pig cerebellum, thus making this region unsuitable as a reference region for in vivo data analysis in this species. The cortical binding of [(18) F]MH.MZ and [(18) F]altanserin was blocked by ketanserin supporting that both radioligands bind to 5-HT(2A) receptors in the pig brain. In the HPLC analysis of pig plasma, [(18) F]MH.MZ displayed a fast and reproducible metabolism resulting in hydrophilic radiometabolites only whereas the metabolic profile of [(18) F]altanserin as expected showed lipophilic radiometabolites. Due to the slow kinetics of [(18) F]MH.MZ in high binding regions in vivo, we suggest that [(18) F]MH.MZ will be an appropriate tracer for low binding regions where kinetics will be faster, whereas [(18) F]altanserin is a suitable tracer for high binding regions. Synapse, 2013. © 2013 Wiley Periodicals, Inc.
Original languageEnglish
JournalSynapse (New York)
Volume67
Issue number6
Pages (from-to)328-37
ISSN0887-4476
DOIs
Publication statusPublished - 2013

ID: 36841276