Specific in vivo binding in the rat brain of [18F]RP 62203: A selective 5-HT2A receptor radioligand for positron emission tomography
| Autor: | François Dauphin, Patrick Mickala, Richard Vivet, Cécile Huard, Laurent Besret, Alexandra Barbelivien, Marie‐Claire Lasne, Jean-Claude Baron |
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| Rok vydání: | 1996 |
| Předmět: |
Male
Fluorine Radioisotopes Cancer Research medicine.drug_class Adrenergic beta-Antagonists Ritanserin Naphthalenes Pharmacology Rats Sprague-Dawley Radioligand Assay In vivo medicine Radioligand Animals Tissue Distribution Radiology Nuclear Medicine and imaging Receptor 5-HT receptor Chemistry Dopaminergic Antagonist Brain Receptor antagonist Cyclic S-Oxides Rats Isotope Labeling Receptors Serotonin Molecular Medicine Serotonin Antagonists Tomography Emission-Computed medicine.drug |
| Zdroj: | Nuclear Medicine and Biology. 23:169-171 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/0969-8051(95)02008-x |
| Popis: | In vivo pharmacokinetic and brain binding characteristics of [ 18 F]RP 62203, a selective high-affinity serotonergic 5-HT 2A receptor antagonist, were assessed in the rat following intravenous injection of trace amount of the radioligand. The radioactive distribution profile observed in the brain 60 min after injection was characterized by greater than fourfold higher uptake in neocortex as compared to cerebellum (0.38 ± 0.07% injected dose/g, % ID/g and 0.08 ± 0.01 ID/g, respectively), consistent with in vivo specific binding to the 5-HT 2A receptor. Furthermore, specific [ 18 F]RP 62203 binding significantly correlated with the reported in vitro distribution of 5-HT 2A receptors, but not with known concentration profiles of dopaminergic D 2 or adrenergic α 1 receptors. Finally, detectable specific binding was abolished by pretreatment with large doses of ritanserin, a selective 5-HT 2A antagonist, which resulted in uniform uptakes across cortical, striatal and cerebellar tissues. Thus, [ 18 F]RP 62203 appears to be a promising selective tool to visualize and quantify 5-HT 2A brain receptors in vivo with positron emission tomography. |
| Databáze: | OpenAIRE |
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