Dopamine D1 receptor imaging in the rodent and primate brain using the isoquinoline (+)‐[11C]A‐69024 and positron emission tomography
Identifieur interne : 008843 ( Main/Exploration ); précédent : 008842; suivant : 008844Dopamine D1 receptor imaging in the rodent and primate brain using the isoquinoline (+)‐[11C]A‐69024 and positron emission tomography
Auteurs : Laurent Besret [France] ; Frédéric Dollé [France] ; Anne-Sophie Hérard [France] ; Martine Guillermier [France] ; Stéphane Demphel [France] ; Françoise Hinnen [France] ; Christine Coulon [France] ; Michèle Ottaviani [France] ; Michel Bottlaender [France] ; Philippe Hantraye [France] ; Michael Kassiou [Australie]Source :
- Journal of Pharmaceutical Sciences [ 0022-3549 ] ; 2008-07.
Descripteurs français
- Pascal (Inist)
- Wicri :
- topic : Radioactivité.
English descriptors
- KwdEn :
- Animal, Arterial blood samples, Attenuation correction, Baboon, Basal ganglia, Binding sites, Biological activity, Biological receptor, Brain regions, Brain structure, Brain uptake, Caudate nucleus, Cerebellar, Cerebellum, Cerebellum ratio, Cobra autogamma, Compds, Contiguous planes, Cortical areas, Cortical regions, D1 Dopamine receptor, Displacement experiment, Displacement study, Dopamine, Dopamine transporter, Emission tomography, Enantiomer, Encephalon, Femoral artery, Frontal cortex, Gamma counter, Hippocampus, Imaging, Intermediate binding, July, Label compds radiopharm, Ligand, Lowest uptake, Medical imagery, Other brain regions, Pharmaceutical, Pharmaceutical sciences, Pharmaceutical technology, Pharmacokinetics, Positron emission tomography, Presaturation experiment, Presaturation studies, Primate brain, Primates, Putamen, Radiat isot, Radioactivity, Radioligand, Radiopharm, Radiotracer, Rapid washout, Receptor, Regional distribution, Rodentia, Selective radioligand, Stereotactic frame, Striatum, Trace amounts, Tracer, Transmission scan, Uptake, Various brain regions, Vivo, Vivo binding, Vivo evaluation.
- Teeft :
- Arterial blood samples, Attenuation correction, Baboon, Basal ganglia, Binding sites, Brain regions, Brain structure, Brain uptake, Caudate nucleus, Cerebellar, Cerebellum, Cerebellum ratio, Cobra autogamma, Compds, Contiguous planes, Cortical areas, Cortical regions, Displacement experiment, Displacement study, Dopamine, Dopamine transporter, Enantiomer, Femoral artery, Frontal cortex, Gamma counter, Hippocampus, Imaging, Intermediate binding, July, Label compds radiopharm, Ligand, Lowest uptake, Other brain regions, Pharmaceutical, Pharmaceutical sciences, Positron emission tomography, Presaturation experiment, Presaturation studies, Primate brain, Putamen, Radiat isot, Radioactivity, Radioligand, Radiopharm, Radiotracer, Rapid washout, Receptor, Regional distribution, Selective radioligand, Stereotactic frame, Striatum, Trace amounts, Tracer, Transmission scan, Uptake, Various brain regions, Vivo, Vivo binding, Vivo evaluation.
Abstract
In vivo pharmacokinetic and brain binding characteristics of (+)‐[11C]A‐69024, a high‐affinity‐D1‐selective dopamine receptor antagonist, were assessed with micro‐PET and β‐microprobes in the rat and PET in the baboon. The biodistribution of (+)‐[11C]A‐69024 in rats and baboons showed a rapid brain uptake (reaching a maximal value at 5 and 15 min postinjection in rats and baboons, respectively), followed by a slow wash out. The region/cerebellum concentration ratio was characterized by a fourfold higher uptake in striatum and a twofold higher uptake in cortical regions, consistent with in vivo specific binding of the radiotracer in these cerebral regions. Furthermore, this specific (+)‐[11C]A‐69024 binding significantly correlated with the reported in vitro distribution of dopamine D1‐receptors. Finally, the specific uptake of the tracer in the striatum and cortical regions was completely prevented by either a pretreatment with large doses of nonradioactive (±)A‐69024 or of the D1‐selective antagonist SCH23390, resulting in a similar uptake in the reference region (cerebellum) and in other brain regions. Thus, (+)‐[11C]A‐69024 appears to be a specific and enantioselective radioligand to visualize and quantify brain dopamine D1 receptors in vivo using positron emission tomography. © 2007 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:2811–2819, 2008
Url:
DOI: 10.1002/jps.21168
Affiliations:
- Australie, France
- Nouvelle-Galles du Sud, Île-de-France
- Fontenay‐aux‐Roses, Orsay, Sydney
- Université de Sydney
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Le document en format XML
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Institute, University of Sydney, Sydney, NSW 2050</wicri:regionArea><orgName type="university">Université de Sydney</orgName><placeName><settlement type="city">Sydney</settlement><region type="état">Nouvelle-Galles du Sud</region></placeName></affiliation><affiliation wicri:level="4"><country xml:lang="fr">Australie</country><wicri:regionArea>School of Chemistry, University of Sydney, Sydney, NSW 2006</wicri:regionArea><orgName type="university">Université de Sydney</orgName><placeName><settlement type="city">Sydney</settlement><region type="état">Nouvelle-Galles du Sud</region></placeName></affiliation><affiliation wicri:level="1"><country wicri:rule="url">Australie</country></affiliation><affiliation wicri:level="4"><orgName type="university">Université de Sydney</orgName><country>Australie</country><placeName><settlement type="city">Sydney</settlement><region type="état">Nouvelle-Galles du Sud</region></placeName></affiliation></author></analytic><monogr></monogr><series><title level="j" type="main">Journal of Pharmaceutical Sciences</title><title level="j" type="alt">JOURNAL OF PHARMACEUTICAL SCIENCES</title><idno type="ISSN">0022-3549</idno><idno type="eISSN">1520-6017</idno><imprint><biblScope unit="vol">97</biblScope><biblScope unit="issue">7</biblScope><biblScope unit="page" from="2811">2811</biblScope><biblScope unit="page" to="2819">2819</biblScope><biblScope unit="page-count">9</biblScope><publisher>Wiley Subscription Services, Inc., A Wiley Company</publisher><pubPlace>Hoboken</pubPlace><date type="published" when="2008-07">2008-07</date></imprint><idno type="ISSN">0022-3549</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-3549</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animal</term><term>Arterial blood samples</term><term>Attenuation correction</term><term>Baboon</term><term>Basal ganglia</term><term>Binding sites</term><term>Biological activity</term><term>Biological receptor</term><term>Brain regions</term><term>Brain structure</term><term>Brain uptake</term><term>Caudate nucleus</term><term>Cerebellar</term><term>Cerebellum</term><term>Cerebellum ratio</term><term>Cobra autogamma</term><term>Compds</term><term>Contiguous planes</term><term>Cortical areas</term><term>Cortical regions</term><term>D1 Dopamine receptor</term><term>Displacement experiment</term><term>Displacement study</term><term>Dopamine</term><term>Dopamine transporter</term><term>Emission tomography</term><term>Enantiomer</term><term>Encephalon</term><term>Femoral artery</term><term>Frontal cortex</term><term>Gamma counter</term><term>Hippocampus</term><term>Imaging</term><term>Intermediate binding</term><term>July</term><term>Label compds radiopharm</term><term>Ligand</term><term>Lowest uptake</term><term>Medical imagery</term><term>Other brain regions</term><term>Pharmaceutical</term><term>Pharmaceutical sciences</term><term>Pharmaceutical technology</term><term>Pharmacokinetics</term><term>Positron emission tomography</term><term>Presaturation experiment</term><term>Presaturation studies</term><term>Primate brain</term><term>Primates</term><term>Putamen</term><term>Radiat isot</term><term>Radioactivity</term><term>Radioligand</term><term>Radiopharm</term><term>Radiotracer</term><term>Rapid washout</term><term>Receptor</term><term>Regional distribution</term><term>Rodentia</term><term>Selective radioligand</term><term>Stereotactic frame</term><term>Striatum</term><term>Trace amounts</term><term>Tracer</term><term>Transmission scan</term><term>Uptake</term><term>Various brain regions</term><term>Vivo</term><term>Vivo binding</term><term>Vivo evaluation</term></keywords><keywords scheme="Pascal" xml:lang="fr"><term>Activité biologique</term><term>Animal</term><term>Encéphale</term><term>Imagerie médicale</term><term>Pharmacocinétique</term><term>Primates</term><term>Rodentia</term><term>Récepteur biologique</term><term>Récepteur dopaminergique D1</term><term>Technologie pharmaceutique</term><term>Tomoscintigraphie</term></keywords><keywords scheme="Teeft" xml:lang="en"><term>Arterial blood samples</term><term>Attenuation correction</term><term>Baboon</term><term>Basal ganglia</term><term>Binding sites</term><term>Brain regions</term><term>Brain structure</term><term>Brain uptake</term><term>Caudate nucleus</term><term>Cerebellar</term><term>Cerebellum</term><term>Cerebellum ratio</term><term>Cobra autogamma</term><term>Compds</term><term>Contiguous planes</term><term>Cortical areas</term><term>Cortical regions</term><term>Displacement experiment</term><term>Displacement study</term><term>Dopamine</term><term>Dopamine transporter</term><term>Enantiomer</term><term>Femoral artery</term><term>Frontal cortex</term><term>Gamma counter</term><term>Hippocampus</term><term>Imaging</term><term>Intermediate binding</term><term>July</term><term>Label compds radiopharm</term><term>Ligand</term><term>Lowest uptake</term><term>Other brain regions</term><term>Pharmaceutical</term><term>Pharmaceutical sciences</term><term>Positron emission tomography</term><term>Presaturation experiment</term><term>Presaturation studies</term><term>Primate brain</term><term>Putamen</term><term>Radiat isot</term><term>Radioactivity</term><term>Radioligand</term><term>Radiopharm</term><term>Radiotracer</term><term>Rapid washout</term><term>Receptor</term><term>Regional distribution</term><term>Selective radioligand</term><term>Stereotactic frame</term><term>Striatum</term><term>Trace amounts</term><term>Tracer</term><term>Transmission scan</term><term>Uptake</term><term>Various brain regions</term><term>Vivo</term><term>Vivo binding</term><term>Vivo evaluation</term></keywords><keywords scheme="Wicri" type="topic" xml:lang="fr"><term>Radioactivité</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">In vivo pharmacokinetic and brain binding characteristics of (+)‐[11C]A‐69024, a high‐affinity‐D1‐selective dopamine receptor antagonist, were assessed with micro‐PET and β‐microprobes in the rat and PET in the baboon. The biodistribution of (+)‐[11C]A‐69024 in rats and baboons showed a rapid brain uptake (reaching a maximal value at 5 and 15 min postinjection in rats and baboons, respectively), followed by a slow wash out. The region/cerebellum concentration ratio was characterized by a fourfold higher uptake in striatum and a twofold higher uptake in cortical regions, consistent with in vivo specific binding of the radiotracer in these cerebral regions. Furthermore, this specific (+)‐[11C]A‐69024 binding significantly correlated with the reported in vitro distribution of dopamine D1‐receptors. Finally, the specific uptake of the tracer in the striatum and cortical regions was completely prevented by either a pretreatment with large doses of nonradioactive (±)A‐69024 or of the D1‐selective antagonist SCH23390, resulting in a similar uptake in the reference region (cerebellum) and in other brain regions. Thus, (+)‐[11C]A‐69024 appears to be a specific and enantioselective radioligand to visualize and quantify brain dopamine D1 receptors in vivo using positron emission tomography. © 2007 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:2811–2819, 2008</div></front></TEI><affiliations><list><country><li>Australie</li><li>France</li></country><region><li>Nouvelle-Galles du Sud</li><li>Île-de-France</li></region><settlement><li>Fontenay‐aux‐Roses</li><li>Orsay</li><li>Sydney</li></settlement><orgName><li>Université de Sydney</li></orgName></list><tree><country name="France"><region name="Île-de-France"><name sortKey="Besret, Laurent" sort="Besret, Laurent" uniqKey="Besret L" first="Laurent" last="Besret">Laurent Besret</name></region><name sortKey="Bottlaender, Michel" sort="Bottlaender, Michel" uniqKey="Bottlaender M" first="Michel" last="Bottlaender">Michel Bottlaender</name><name sortKey="Coulon, Christine" sort="Coulon, Christine" uniqKey="Coulon C" first="Christine" last="Coulon">Christine Coulon</name><name sortKey="Demphel, Stephane" sort="Demphel, Stephane" uniqKey="Demphel S" first="Stéphane" last="Demphel">Stéphane Demphel</name><name sortKey="Dolle, Frederic" sort="Dolle, Frederic" uniqKey="Dolle F" first="Frédéric" last="Dollé">Frédéric Dollé</name><name sortKey="Guillermier, Martine" sort="Guillermier, Martine" uniqKey="Guillermier M" first="Martine" last="Guillermier">Martine Guillermier</name><name sortKey="Guillermier, Martine" sort="Guillermier, Martine" uniqKey="Guillermier M" first="Martine" last="Guillermier">Martine Guillermier</name><name sortKey="Hantraye, Philippe" sort="Hantraye, Philippe" uniqKey="Hantraye P" first="Philippe" last="Hantraye">Philippe Hantraye</name><name sortKey="Hantraye, Philippe" sort="Hantraye, Philippe" uniqKey="Hantraye P" first="Philippe" last="Hantraye">Philippe Hantraye</name><name sortKey="Herard, Anne Ophie" sort="Herard, Anne Ophie" uniqKey="Herard A" first="Anne-Sophie" last="Hérard">Anne-Sophie Hérard</name><name sortKey="Herard, Anne Ophie" sort="Herard, Anne Ophie" uniqKey="Herard A" first="Anne-Sophie" last="Hérard">Anne-Sophie Hérard</name><name sortKey="Hinnen, Francoise" sort="Hinnen, Francoise" uniqKey="Hinnen F" first="Françoise" last="Hinnen">Françoise Hinnen</name><name sortKey="Ottaviani, Michele" sort="Ottaviani, Michele" uniqKey="Ottaviani M" first="Michèle" last="Ottaviani">Michèle Ottaviani</name></country><country name="Australie"><region name="Nouvelle-Galles du Sud"><name sortKey="Kassiou, Michael" sort="Kassiou, Michael" uniqKey="Kassiou M" first="Michael" last="Kassiou">Michael Kassiou</name></region><name sortKey="Kassiou, Michael" sort="Kassiou, Michael" uniqKey="Kassiou M" first="Michael" last="Kassiou">Michael Kassiou</name><name sortKey="Kassiou, Michael" sort="Kassiou, Michael" uniqKey="Kassiou M" first="Michael" last="Kassiou">Michael Kassiou</name><name sortKey="Kassiou, Michael" sort="Kassiou, Michael" uniqKey="Kassiou M" first="Michael" last="Kassiou">Michael Kassiou</name><name sortKey="Kassiou, Michael" sort="Kassiou, Michael" uniqKey="Kassiou M" first="Michael" last="Kassiou">Michael Kassiou</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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