In vivo binding properties of [carbonyl‐11C]WAY‐100635: Effect of endogenous serotonin
- 8 March 2001
- Vol. 40 (2) , 122-129
- https://doi.org/10.1002/syn.1033
Abstract
[Carbonyl-11C]WAY-100635 has been reported to be a useful ligand for the investigation of 5-HT1A receptor imaging in vivo. However, the cellular distribution and the influence of endogenous serotonin (5-HT) on in vivo binding have not been fully examined. In this study, we investigated the effect of 5,7-dihydroxytryptamine-produced destruction of 5-HT neurons, reserpine-induced 5-HT depletion, and fenfluramine-induced 5-HT increase on [carbonyl-11C]WAY-100635 binding in vivo. There was no significant change in the uptake of [carbonyl-11C]WAY-100635 in the slice of 5-HT denervated rat brain except in the raphe nucleus, where 5-HT cell bodies exist. There was no obvious effect of enhanced 5-HT release by fenfluramine or decreased release by reserpine on [carbonyl-11C]WAY-100635 binding in the dissected brain region. No significant effect was observed in the time course of [carbonyl-11C]WAY-100635 in the hippocampus and frontal cortex measured by PET. These results indicated that the in vivo binding of [carbonyl-11C]WAY-100635 in the hippocampus and cerebral cortex mainly reflects postsynaptic 5-HT1A receptor binding, and that this binding is not sensitive to endogenous 5-HT. Synapse 40:122–129, 2001.Keywords
This publication has 32 references indexed in Scilit:
- The selective 5-HT1A antagonist radioligand [3H]WAY 100635 labels both G-protein-coupled and free 5-HT1A receptors in rat brain membranesPublished by Elsevier ,2003
- Assessment of Dynamic Neurotransmitter Changes with Bolus or Infusion Delivery of Neuroreceptor LigandsJournal of Cerebral Blood Flow & Metabolism, 1998
- Effect of reserpine-induced depletion of synaptic dopamine on [11C]Raclopride binding to D2-dopamine receptors in the monkey brainSynapse, 1997
- Cellular localization of the 5-HT1A receptor in primate brain neurons and glial cellsNeuropsychopharmacology, 1996
- Depletion and repletion of cortical tissue and dialysate 5-HT after reserpineNeuropharmacology, 1994
- Localization of 5‐HT1A receptors to astroglial cells in adult rats: Implications for neuronal‐glial interactions and psychoactive drug mechanism of actionSynapse, 1993
- Quantitation of Carbon‐11‐labeled raclopride in rat striatum using positron emission tomographySynapse, 1992
- Sub-types of serotonin receptorsInternational Clinical Psychopharmacology, 1992
- Difference in in vivo receptor binding between [3 H]N-methylspiperone and [3 H]raclopride in reserpine-treated mouse brainJournal Of Neural Transmission-Parkinsons Disease and Dementia Section, 1991
- Kinetic Analysis of Central [11C]Raclopride Binding to D2-Dopamine Receptors Studied by PET—A Comparison to the Equilibrium AnalysisJournal of Cerebral Blood Flow & Metabolism, 1989