Preclinical in vivo and in vitro comparison of the translocator protein PET ligands [(18)F]PBR102 and [(18)F]PBR111.
Identifieur interne : 003C54 ( Ncbi/Merge ); précédent : 003C53; suivant : 003C55Preclinical 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
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pubmed:27699720Le document en format XML
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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><pubmed><MedlineCitation Status="MEDLINE" Owner="NLM"><PMID Version="1">27699720</PMID><DateCreated><Year>2016</Year><Month>10</Month><Day>04</Day></DateCreated><DateCompleted><Year>2017</Year><Month>03</Month><Day>06</Day></DateCompleted><DateRevised><Year>2017</Year><Month>09</Month><Day>26</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1619-7089</ISSN><JournalIssue CitedMedium="Internet"><Volume>44</Volume><Issue>2</Issue><PubDate><Year>2017</Year><Month>Feb</Month></PubDate></JournalIssue><Title>European journal of nuclear medicine and molecular imaging</Title><ISOAbbreviation>Eur. J. Nucl. Med. Mol. Imaging</ISOAbbreviation></Journal><ArticleTitle>Preclinical in vivo and in vitro comparison of the translocator protein PET ligands [(18)F]PBR102 and [(18)F]PBR111.</ArticleTitle><Pagination><MedlinePgn>296-307</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1007/s00259-016-3517-z</ELocationID><Abstract><AbstractText Label="PURPOSE" NlmCategory="OBJECTIVE">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.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">In vitro metabolic profiles of PBR102 and PBR111 in rat and human liver microsomes were assessed by liquid chromatography-tandem mass spectrometry. [(18)F]PBR102 and [(18)F]PBR111 were prepared by nucleophilic substitution of their corresponding p-toluenesulfonyl precursors with [(18)F]fluoride. List mode PET-CT brain imaging with arterial blood sampling was performed in non-human primates. Blood plasma measurements and metabolite analysis, using solid-phase extraction, provided the metabolite profile and metabolite-corrected input functions for kinetic model fitting. Blocking and displacement PET-CT scans, using PK11195, were performed.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Microsomal analyses identified the O-de-alkylated, hydroxylated and N-de-ethyl derivatives of PBR102 and PBR111 as the main metabolites. The O-de-alkylated compounds were the major metabolites in both species; human liver microsomes were less active than those from rat. Metabolic profiles in vivo in non-human primates and previously published rat experiments were consistent with the microsomal results. PET-CT studies showed that K1 was similar for baseline and blocking studies for both radiotracers; VT was reduced during the blocking study, suggesting low non-specific binding and lack of appreciable metabolite uptake in the brain.</AbstractText><AbstractText Label="CONCLUSIONS" NlmCategory="CONCLUSIONS">[(18)F]PBR102 and [(18)F]PBR111 have distinct metabolic profiles in rat and non-human primates. Radiometabolites contributed to non-specific binding and confounded in vivo brain analysis of [(18)F]PBR102 in rodents; the impact in primates was less pronounced. Both [(18)F]PBR102 and [(18)F]PBR111 are suitable for PET imaging of TSPO in vivo. In vitro metabolite studies can be used to predict in vivo radioligand metabolism and can assist in the design and development of better radioligands.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Eberl</LastName><ForeName>S</ForeName><Initials>S</Initials><AffiliationInfo><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.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Faculty of Engineering and Information Technologies, University of Sydney, Sydney, NSW, 2006, Australia. stefan.eberl@sydney.edu.au.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Katsifis</LastName><ForeName>A</ForeName><Initials>A</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Faculty of Pharmacy, University of Sydney, Sydney, NSW, 2006, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Peyronneau</LastName><ForeName>M A</ForeName><Initials>MA</Initials><AffiliationInfo><Affiliation>IMIV, CEA, Inserm, Univ. Paris-Sud, CNRS, Université Paris-Saclay, CEA-SHFJ, Orsay, France.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Wen</LastName><ForeName>L</ForeName><Initials>L</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Faculty of Engineering and Information Technologies, University of Sydney, Sydney, NSW, 2006, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Henderson</LastName><ForeName>D</ForeName><Initials>D</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Loc'h</LastName><ForeName>C</ForeName><Initials>C</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Greguric</LastName><ForeName>I</ForeName><Initials>I</Initials><AffiliationInfo><Affiliation>Radiochemistry and Radiotracers Platform, ANSTO, New Illawarra Road, Lucas Heights, NSW, 2234, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Verschuer</LastName><ForeName>J</ForeName><Initials>J</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Pham</LastName><ForeName>T</ForeName><Initials>T</Initials><AffiliationInfo><Affiliation>Radiochemistry and Radiotracers Platform, ANSTO, New Illawarra Road, Lucas Heights, NSW, 2234, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Lam</LastName><ForeName>P</ForeName><Initials>P</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Mattner</LastName><ForeName>F</ForeName><Initials>F</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Mohamed</LastName><ForeName>A</ForeName><Initials>A</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Sydney Medical School, University of Sydney, Sydney, NSW, 2006, Australia.</Affiliation></AffiliationInfo></Author><Author ValidYN="Y"><LastName>Fulham</LastName><ForeName>M J</ForeName><Initials>MJ</Initials><AffiliationInfo><Affiliation>Department of Molecular Imaging (PET and Nuclear Medicine), Royal Prince Alfred Hospital, Building 63, Level A7, Missenden Road, Camperdown, NSW, 2050, Australia.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Faculty of Engineering and Information Technologies, University of Sydney, Sydney, NSW, 2006, Australia.</Affiliation></AffiliationInfo><AffiliationInfo><Affiliation>Sydney Medical School, University of Sydney, Sydney, NSW, 2006, Australia.</Affiliation></AffiliationInfo></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType UI="D003160">Comparative Study</PublicationType><PublicationType UI="D016428">Journal Article</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2016</Year><Month>10</Month><Day>04</Day></ArticleDate></Article><MedlineJournalInfo><Country>Germany</Country><MedlineTA>Eur J Nucl Med Mol Imaging</MedlineTA><NlmUniqueID>101140988</NlmUniqueID><ISSNLinking>1619-7070</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="C576229">2-(6-chloro-2-(4-(2-fluoroethoxy)phenyl)imidazo(1,2-a)pyridin-3-yl)-N,N-diethylacetamide</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="C550561">2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo(1,2-a)pyridin-3-yl)-N,N-diethylacetamide</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D007093">Imidazoles</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D008024">Ligands</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D011725">Pyridines</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D019275">Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="D018079">Receptors, GABA</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance UI="C499229">TSPO protein, human</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><CommentsCorrectionsList><CommentsCorrections RefType="Cites"><RefSource>Nat Rev Drug Discov. 2010 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Version="1">22841687</PMID></CommentsCorrections></CommentsCorrectionsList><MeshHeadingList><MeshHeading><DescriptorName UI="D000818" MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D001921" MajorTopicYN="N">Brain</DescriptorName><QualifierName UI="Q000000981" MajorTopicYN="N">diagnostic imaging</QualifierName><QualifierName UI="Q000378" MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D004353" MajorTopicYN="N">Drug Evaluation, Preclinical</DescriptorName><QualifierName UI="Q000379" MajorTopicYN="N">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D006801" MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D007093" MajorTopicYN="N">Imidazoles</DescriptorName><QualifierName UI="Q000493" MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D007553" MajorTopicYN="N">Isotope Labeling</DescriptorName><QualifierName UI="Q000379" MajorTopicYN="N">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D008024" MajorTopicYN="N">Ligands</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D008297" MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D008657" MajorTopicYN="N">Metabolic Clearance Rate</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D057054" MajorTopicYN="N">Molecular Imaging</DescriptorName><QualifierName UI="Q000379" MajorTopicYN="Y">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D009928" MajorTopicYN="N">Organ Specificity</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D010215" MajorTopicYN="N">Papio</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D049268" MajorTopicYN="N">Positron-Emission Tomography</DescriptorName><QualifierName UI="Q000379" MajorTopicYN="Y">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D011725" MajorTopicYN="N">Pyridines</DescriptorName><QualifierName UI="Q000493" MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D019275" MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName UI="Q000138" MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName UI="Q000493" MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D051381" MajorTopicYN="N">Rats</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D018079" MajorTopicYN="N">Receptors, GABA</DescriptorName><QualifierName UI="Q000378" MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName UI="D015203" MajorTopicYN="N">Reproducibility of Results</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D012680" MajorTopicYN="N">Sensitivity and Specificity</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D013045" MajorTopicYN="N">Species Specificity</DescriptorName></MeshHeading><MeshHeading><DescriptorName UI="D014018" MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading></MeshHeadingList><KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="Y">Metabolism</Keyword><Keyword MajorTopicYN="Y">Microsomes</Keyword><Keyword MajorTopicYN="Y">Non-human primate PET-CT</Keyword><Keyword MajorTopicYN="Y">TSPO</Keyword><Keyword MajorTopicYN="Y">[18F]PBR102</Keyword><Keyword MajorTopicYN="Y">[18F]PBR111</Keyword></KeywordList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2016</Year><Month>05</Month><Day>30</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2016</Year><Month>09</Month><Day>05</Day></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2016</Year><Month>10</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2017</Year><Month>3</Month><Day>7</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2016</Year><Month>10</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">27699720</ArticleId><ArticleId IdType="doi">10.1007/s00259-016-3517-z</ArticleId><ArticleId IdType="pii">10.1007/s00259-016-3517-z</ArticleId></ArticleIdList></PubmedData></pubmed><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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