Toward brain imaging of serotonin 5-HT1A autoreceptor internalization

NeuroImage
Luc ZimmerLaurent Descarries

Abstract

Enhancing cerebral serotonin (5-hydroxytryptamine, 5-HT) neurotransmission is a common property of antidepressant treatments and the basis for their efficacy. 5-HT1A receptors located on the cell body and dendrites of 5-HT neurons (autoreceptors) play a key role in this regard. Because they normally mediate an inhibition of neuronal firing, their desensitization is a prerequisite to the delayed enhancement of 5-HT neurotransmission upon treatment with monoamine oxidase (MAOI) inhibitors or specific serotonin reuptake inhibitors (SSRI). Using beta-sensitive microprobes in vivo, we measured a significant decrease (-30%) in binding sites for the 5-HT1A PET radioligand [18F]MPPF associated with an equivalent reduction (-34%) in the cell surface density of 5-HT1A receptor immunoreactivity (internalization), in the nucleus raphe dorsalis (autoreceptors), but not hippocampus (heteroreceptors), of rats given a single dose of the specific 5-HT1A receptor agonist, 8-OH-DPAT (0.5 mg/kg, iv). This effect was completely blocked by pretreatment with the selective 5-HT1A antagonist WAY 100635. Having ruled out that this decreased density of [18F]MPPF binding in the nucleus raphe dorsalis of 8-OH-DPAT-treated rats resulted from a local blood f...Continue Reading

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Citations

Aug 16, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Nicolas AznavourLaurent Descarries
Jul 25, 2013·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Shigeyuki YamamotoEdward F Domino
Jul 25, 2012·Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences·Laurent Descarries, Mustaph Riad
Jun 23, 2006·Anesthesia and Analgesia·Robert A Whittington, László Virág
May 12, 2009·Progress in Neurobiology·Jonathan SavitzWayne C Drevets
Jul 29, 2010·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Louise M PatersonGitte M Knudsen
Mar 7, 2006·Journal of Chemical Neuroanatomy·Nicolas AznavourLuc Zimmer
Oct 19, 2004·Radiologic Clinics of North America·Chyng-Yann Shiue, Michael J Welch
Feb 18, 2005·The Journal of Pharmacology and Experimental Therapeutics·Chris R GuthrieMark W Hamblin
Nov 5, 2019·Frontiers in Molecular Neuroscience·Matthieu ColomLuc Zimmer
Mar 26, 2021·Frontiers in Neuroscience·Matthieu ColomLuc Zimmer
Jun 17, 2008·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Aurélie DesbréePhilippe Lanièce
Nov 15, 2006·Neuropharmacology·Nicolas Aznavour, Luc Zimmer
Mar 22, 2019·Biochemistry·G Aditya KumarAmitabha Chattopadhyay

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