Preclinical in vivo and in vitro comparison of the translocator protein PET ligands [(18)F]PBR102 and [(18)F]PBR111.
Identifieur interne : 000581 ( Main/Exploration ); précédent : 000580; suivant : 000582Preclinical in vivo and in vitro comparison of the translocator protein PET ligands [(18)F]PBR102 and [(18)F]PBR111.
Auteurs : S. Eberl [Australie] ; A. Katsifis [Australie] ; M A Peyronneau [France] ; L. Wen [Australie] ; D. Henderson [Australie] ; C. Loc'H [Australie] ; I. Greguric [Australie] ; J. Verschuer [Australie] ; T. Pham [Australie] ; P. Lam [Australie] ; F. Mattner [Australie] ; A. Mohamed [Australie] ; M J Fulham [Australie]Source :
- European journal of nuclear medicine and molecular imaging [ 1619-7089 ] ; 2017.
Descripteurs français
- KwdFr :
- Animaux, Clairance métabolique, Encéphale (imagerie diagnostique), Encéphale (métabolisme), Humains, Imagerie moléculaire (), Imidazoles (pharmacocinétique), Ligands, Marquage isotopique (), Mâle, Papio, Pyridines (pharmacocinétique), Radiopharmaceutiques (pharmacocinétique), Radiopharmaceutiques (synthèse chimique), Rats, Reproductibilité des résultats, Récepteurs GABA (métabolisme), Répartition dans les tissus, Sensibilité et spécificité, Spécificité d'espèce, Spécificité d'organe, Tomographie par émission de positons (), Évaluation préclinique de médicament ().
- MESH :
- imagerie diagnostique : Encéphale.
- métabolisme : Encéphale, Récepteurs GABA.
- pharmacocinétique : Imidazoles, Pyridines, Radiopharmaceutiques.
- synthèse chimique : Radiopharmaceutiques.
- Animaux, Clairance métabolique, Humains, Imagerie moléculaire, Ligands, Marquage isotopique, Mâle, Papio, Rats, Reproductibilité des résultats, Répartition dans les tissus, Sensibilité et spécificité, Spécificité d'espèce, Spécificité d'organe, Tomographie par émission de positons, Évaluation préclinique de médicament.
English descriptors
- KwdEn :
- Animals, Brain (diagnostic imaging), Brain (metabolism), Drug Evaluation, Preclinical (methods), Humans, Imidazoles (pharmacokinetics), Isotope Labeling (methods), Ligands, Male, Metabolic Clearance Rate, Molecular Imaging (methods), Organ Specificity, Papio, Positron-Emission Tomography (methods), Pyridines (pharmacokinetics), Radiopharmaceuticals (chemical synthesis), Radiopharmaceuticals (pharmacokinetics), Rats, Receptors, GABA (metabolism), Reproducibility of Results, Sensitivity and Specificity, Species Specificity, Tissue Distribution.
- MESH :
- chemical , chemical synthesis : Radiopharmaceuticals.
- chemical , metabolism : Receptors, GABA.
- chemical , pharmacokinetics : Imidazoles, Pyridines, Radiopharmaceuticals.
- diagnostic imaging : Brain.
- metabolism : Brain.
- methods : Drug Evaluation, Preclinical, Isotope Labeling, Molecular Imaging, Positron-Emission Tomography.
- Animals, Humans, Ligands, Male, Metabolic Clearance Rate, Organ Specificity, Papio, Rats, Reproducibility of Results, Sensitivity and Specificity, Species Specificity, Tissue Distribution.
Abstract
To determine the metabolic profiles of the translocator protein ligands PBR102 and PBR111 in rat and human microsomes and compare their in vivo binding and metabolite uptake in the brain of non-human primates (Papio hamadryas) using PET-CT.
DOI: 10.1007/s00259-016-3517-z
PubMed: 27699720
Affiliations:
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Eberl</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia. stefan.eberl@sydney.edu.au.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Katsifis, A" sort="Katsifis, A" uniqKey="Katsifis A" first="A" last="Katsifis">A. Katsifis</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Peyronneau, M A" sort="Peyronneau, M A" uniqKey="Peyronneau M" first="M A" last="Peyronneau">M A Peyronneau</name><affiliation wicri:level="3"><nlm:affiliation>IMIV, CEA, Inserm, Univ. Paris-Sud, CNRS, Université Paris-Saclay, CEA-SHFJ, Orsay, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>IMIV, CEA, Inserm, Univ. Paris-Sud, CNRS, Université Paris-Saclay, CEA-SHFJ, Orsay</wicri:regionArea><placeName><settlement type="city">Orsay</settlement></placeName></affiliation></author><author><name sortKey="Wen, L" sort="Wen, L" uniqKey="Wen L" first="L" last="Wen">L. Wen</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Henderson, D" sort="Henderson, D" uniqKey="Henderson D" first="D" last="Henderson">D. Henderson</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Loc H, C" sort="Loc H, C" uniqKey="Loc H C" first="C" last="Loc'H">C. Loc'H</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Greguric, I" sort="Greguric, I" uniqKey="Greguric I" first="I" last="Greguric">I. Greguric</name><affiliation wicri:level="1"><nlm:affiliation>Radiochemistry and Radiotracers Platform, ANSTO, New Illawarra Road, Lucas Heights, NSW, 2234, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Radiochemistry and Radiotracers Platform, ANSTO, New Illawarra Road, Lucas Heights, NSW, 2234</wicri:regionArea><wicri:noRegion>2234</wicri:noRegion></affiliation></author><author><name sortKey="Verschuer, J" sort="Verschuer, J" uniqKey="Verschuer J" first="J" last="Verschuer">J. Verschuer</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Pham, T" sort="Pham, T" uniqKey="Pham T" first="T" last="Pham">T. Pham</name><affiliation wicri:level="1"><nlm:affiliation>Radiochemistry and Radiotracers Platform, ANSTO, New Illawarra Road, Lucas Heights, NSW, 2234, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Radiochemistry and Radiotracers Platform, ANSTO, New Illawarra Road, Lucas Heights, NSW, 2234</wicri:regionArea><wicri:noRegion>2234</wicri:noRegion></affiliation></author><author><name sortKey="Lam, P" sort="Lam, P" uniqKey="Lam P" first="P" last="Lam">P. Lam</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Mattner, F" sort="Mattner, F" uniqKey="Mattner F" first="F" last="Mattner">F. Mattner</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Mohamed, A" sort="Mohamed, A" uniqKey="Mohamed A" first="A" last="Mohamed">A. Mohamed</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author><author><name sortKey="Fulham, M J" sort="Fulham, M J" uniqKey="Fulham M" first="M J" last="Fulham">M J Fulham</name><affiliation wicri:level="1"><nlm:affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</nlm:affiliation><country xml:lang="fr">Australie</country><wicri:regionArea>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050</wicri:regionArea><wicri:noRegion>2050</wicri:noRegion></affiliation></author></analytic><series><title level="j">European journal of nuclear medicine and molecular imaging</title><idno type="eISSN">1619-7089</idno><imprint><date when="2017" type="published">2017</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Brain (diagnostic imaging)</term><term>Brain (metabolism)</term><term>Drug Evaluation, Preclinical (methods)</term><term>Humans</term><term>Imidazoles (pharmacokinetics)</term><term>Isotope Labeling (methods)</term><term>Ligands</term><term>Male</term><term>Metabolic Clearance Rate</term><term>Molecular Imaging (methods)</term><term>Organ Specificity</term><term>Papio</term><term>Positron-Emission Tomography (methods)</term><term>Pyridines (pharmacokinetics)</term><term>Radiopharmaceuticals (chemical synthesis)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Rats</term><term>Receptors, GABA (metabolism)</term><term>Reproducibility of Results</term><term>Sensitivity and Specificity</term><term>Species Specificity</term><term>Tissue Distribution</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Clairance métabolique</term><term>Encéphale (imagerie diagnostique)</term><term>Encéphale (métabolisme)</term><term>Humains</term><term>Imagerie moléculaire ()</term><term>Imidazoles (pharmacocinétique)</term><term>Ligands</term><term>Marquage isotopique ()</term><term>Mâle</term><term>Papio</term><term>Pyridines (pharmacocinétique)</term><term>Radiopharmaceutiques (pharmacocinétique)</term><term>Radiopharmaceutiques (synthèse chimique)</term><term>Rats</term><term>Reproductibilité des résultats</term><term>Récepteurs GABA (métabolisme)</term><term>Répartition dans les tissus</term><term>Sensibilité et spécificité</term><term>Spécificité d'espèce</term><term>Spécificité d'organe</term><term>Tomographie par émission de positons ()</term><term>Évaluation préclinique de médicament ()</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Receptors, GABA</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Imidazoles</term><term>Pyridines</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" qualifier="diagnostic imaging" xml:lang="en"><term>Brain</term></keywords><keywords scheme="MESH" qualifier="imagerie diagnostique" xml:lang="fr"><term>Encéphale</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Brain</term></keywords><keywords scheme="MESH" qualifier="methods" xml:lang="en"><term>Drug Evaluation, Preclinical</term><term>Isotope Labeling</term><term>Molecular Imaging</term><term>Positron-Emission Tomography</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Encéphale</term><term>Récepteurs GABA</term></keywords><keywords scheme="MESH" qualifier="pharmacocinétique" xml:lang="fr"><term>Imidazoles</term><term>Pyridines</term><term>Radiopharmaceutiques</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Radiopharmaceutiques</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Humans</term><term>Ligands</term><term>Male</term><term>Metabolic Clearance Rate</term><term>Organ Specificity</term><term>Papio</term><term>Rats</term><term>Reproducibility of Results</term><term>Sensitivity and Specificity</term><term>Species Specificity</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Clairance métabolique</term><term>Humains</term><term>Imagerie moléculaire</term><term>Ligands</term><term>Marquage isotopique</term><term>Mâle</term><term>Papio</term><term>Rats</term><term>Reproductibilité des résultats</term><term>Répartition dans les tissus</term><term>Sensibilité et spécificité</term><term>Spécificité d'espèce</term><term>Spécificité d'organe</term><term>Tomographie par émission de positons</term><term>Évaluation préclinique de médicament</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">To determine the metabolic profiles of the translocator protein ligands PBR102 and PBR111 in rat and human microsomes and compare their in vivo binding and metabolite uptake in the brain of non-human primates (Papio hamadryas) using PET-CT.</div></front></TEI><affiliations><list><country><li>Australie</li><li>France</li></country><settlement><li>Orsay</li></settlement></list><tree><country name="Australie"><noRegion><name sortKey="Eberl, S" sort="Eberl, S" uniqKey="Eberl S" first="S" last="Eberl">S. Eberl</name></noRegion><name sortKey="Fulham, M J" sort="Fulham, M J" uniqKey="Fulham M" first="M J" last="Fulham">M J Fulham</name><name sortKey="Greguric, I" sort="Greguric, I" uniqKey="Greguric I" first="I" last="Greguric">I. Greguric</name><name sortKey="Henderson, D" sort="Henderson, D" uniqKey="Henderson D" first="D" last="Henderson">D. Henderson</name><name sortKey="Katsifis, A" sort="Katsifis, A" uniqKey="Katsifis A" first="A" last="Katsifis">A. Katsifis</name><name sortKey="Lam, P" sort="Lam, P" uniqKey="Lam P" first="P" last="Lam">P. Lam</name><name sortKey="Loc H, C" sort="Loc H, C" uniqKey="Loc H C" first="C" last="Loc'H">C. Loc'H</name><name sortKey="Mattner, F" sort="Mattner, F" uniqKey="Mattner F" first="F" last="Mattner">F. Mattner</name><name sortKey="Mohamed, A" sort="Mohamed, A" uniqKey="Mohamed A" first="A" last="Mohamed">A. Mohamed</name><name sortKey="Pham, T" sort="Pham, T" uniqKey="Pham T" first="T" last="Pham">T. Pham</name><name sortKey="Verschuer, J" sort="Verschuer, J" uniqKey="Verschuer J" first="J" last="Verschuer">J. Verschuer</name><name sortKey="Wen, L" sort="Wen, L" uniqKey="Wen L" first="L" last="Wen">L. Wen</name></country><country name="France"><noRegion><name sortKey="Peyronneau, M A" sort="Peyronneau, M A" uniqKey="Peyronneau M" first="M A" last="Peyronneau">M A Peyronneau</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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