Synthesis and evaluation of 4-(2-fluoro-4-[

Animals Brain / diagnostic imaging Carbon Radioisotopes Dose-Response Relationship, Drug Humans Male Mice Mice, Inbred Strains Mice, Knockout Molecular Structure Picolinic Acids / chemical synthesis Positron-Emission Tomography Radioactive Tracers Rats Rats, Sprague-Dawley Receptors, Metabotropic Glutamate / analysis Structure-Activity Relationship Tissue Distribution
In vitro autoradiography Metabotropic glutamate receptor 2 Positron emission tomography Radiotracer Schizophrenia

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 02 2019
Historique:
received: 12 10 2018
revised: 13 12 2018
accepted: 15 12 2018
pubmed: 7 1 2019
medline: 18 12 2019
entrez: 7 1 2019
Statut: ppublish

Résumé

Metabotropic glutamate receptor 2 (mGluR2) has been suggested as a therapeutic target for treating schizophrenia-like symptoms arising from increased glutamate transmission in the human forebrain. However, no reliable positron emission tomography (PET) radiotracer allowing for in vivo visualization of mGluR2 in the human brain is currently available. In this study, we synthesized 4-(2-fluoro-4-[

Identifiants

DOI: 10.1016/j.bmc.2018.12.025 PMID: 30611634
pubmed: 30611634
pii: S0968-0896(18)31754-1
doi: 10.1016/j.bmc.2018.12.025
pii:
doi:

Substances chimiques

Carbon Radioisotopes 0
Carbon-11 0
Picolinic Acids 0
Radioactive Tracers 0
Receptors, Metabotropic Glutamate 0
metabotropic glutamate receptor 2 0
picolinamide I3550CCL59

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

483-491

Informations de copyright

Copyright © 2018 Elsevier Ltd. All rights reserved.

Auteurs

Katsushi Kumata (K)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Akiko Hatori (A)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Tomoteru Yamasaki (T)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Yiding Zhang (Y)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Wakana Mori (W)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Masayuki Fujinaga (M)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Lin Xie (L)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan.

Nobuki Nengaki (N)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan; SHI Accelerator Services Co., 1-17-6 Osaki, Shinagawa-ku, Tokyo 141-0032, Japan.

Ming-Rong Zhang (MR)

Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan. Electronic address: zhang.ming-rong@qst.go.jp.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Produits chimiques inorganiques › Isotopes › Radio-isotopes › Radio-isotopes du carbone › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Souris transgéniques › Souris knockout › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyridines › Acides picoliniques › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Diagnostic › Techniques et procédures diagnostiques › Techniques de diagnostic radioisotopique › Scintigraphie › Tomoscintigraphie › Tomographie par émission de positons › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Indicateurs et réactifs › Traceurs radioactifs › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Rat Sprague-Dawley › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs au glutamate › Récepteurs métabotropes au glutamate › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Synthesis and evaluation of 4-(2-fluoro-4-[
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Pharmacocinétique › Distribution tissulaire › Synthesis and evaluation of 4-(2-fluoro-4-[