Cerebral 5-HT release correlates with [11C]Cimbi36 PET measures of 5-HT2A receptor occupancy in the pig brain

Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism
Louise M JørgensenGitte M Knudsen

Abstract

Positron emission tomography (PET) can, when used with appropriate radioligands, non-invasively generate temporal and spatial information about acute changes in brain neurotransmitter systems. We for the first time evaluate the novel 5-HT2A receptor agonist PET radioligand, [11C]Cimbi-36, for its sensitivity to detect changes in endogenous cerebral 5-HT levels, as induced by different pharmacological challenges. To enable a direct translation of PET imaging data to changes in brain 5-HT levels, we calibrated the [11C]Cimbi-36 PET signal in the pig brain by simultaneous measurements of extracellular 5-HT levels with microdialysis and [11C]Cimbi-36 PET after various acute interventions (saline, citalopram, citalopram + pindolol, fenfluramine). In a subset of pigs, para-chlorophenylalanine pretreatment was given to deplete cerebral 5-HT. The interventions increased the cerebral extracellular 5-HT levels to 2-11 times baseline, with fenfluramine being the most potent pharmacological enhancer of 5-HT release, and induced a varying degree of decline in [11C]Cimbi-36 binding in the brain, consistent with the occupancy competition model. The observed correlation between changes in the extracellular 5-HT level in the pig brain and the 5...Continue Reading

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Citations

Jul 8, 2017·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Louise M JørgensenGitte M Knudsen
Nov 13, 2019·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·David ErritzoeEugenii A Rabiner
Jan 28, 2019·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Martin K MadsenGitte M Knudsen
Jun 7, 2019·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Kristina HerfertBernd J Pichler
Jul 30, 2019·Frontiers in Physiology·Brendan Hoffe, Matthew R Holahan
Nov 5, 2019·Frontiers in Molecular Neuroscience·Matthieu ColomLuc Zimmer
Mar 26, 2021·Frontiers in Neuroscience·Matthieu ColomLuc Zimmer
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Jul 17, 2021·Biological Psychiatry·Sofi da Cunha-Bang, Gitte Moos Knudsen
Oct 29, 2019·ACS Chemical Neuroscience·Christian B M PoulieJesper L Kristensen

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