Radiosynthesis of (R,S)-[

Animals Fluorine Radioisotopes / chemistry Humans Polymorphism, Genetic Positron-Emission Tomography Proof of Concept Study Protein Binding Radiopharmaceuticals / chemical synthesis Rats Receptors, GABA / chemistry Stereoisomerism
PET imaging TSPO receptor [18F]GE180 [18F]GE387 neuroinflammation biomarkers

Journal

ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013

Informations de publication

Date de publication:
06 05 2019
Historique:
received: 10 01 2019
revised: 26 02 2019
pubmed: 23 3 2019
medline: 18 2 2020
entrez: 23 3 2019
Statut: ppublish

Résumé

Translocator protein (TSPO) is a biomarker of neuroinflammation, which is a hallmark of many neurodegenerative diseases and has been exploited as a positron emission tomography (PET) target. Carbon-11-labelled PK11195 remains the most applied agent for imaging TSPO, despite its short-lived isotope and low brain permeability. Second-generation radiotracers show variance in affinity amongst subjects (low-, mixed-, and high-affinity binders) caused by the genetic polymorphism (rs6971) of the TSPO gene. To overcome these limitations, a new structural scaffold was explored based on the TSPO pharmacophore, and the analogue with a low-affinity binder/high-affinity binder (LAB/HAB) ratio similar (1.2 vs. 1.3) to that of (R)-[

Identifiants

DOI: 10.1002/cmdc.201900023 PMID: 30900397 PMC: PMC6563049
pubmed: 30900397
doi: 10.1002/cmdc.201900023
pmc: PMC6563049
doi:

Substances chimiques

Fluorine Radioisotopes 0
Radiopharmaceuticals 0
Receptors, GABA 0
TSPO protein, human 0

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

982-993

Subventions

Organisme : Medical Research Council
ID : MR/K02308X/1
Pays : United Kingdom
Organisme : Medical Research Council
ID : RG70550
Pays : United Kingdom
Organisme : Department of Health
Pays : United Kingdom
Organisme : Medical Research Council
ID : RG46503
Pays : United Kingdom
Organisme : Medical Research Council
ID : MC_PC_16040
Pays : United Kingdom

Informations de copyright

© 2019 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.

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Auteurs

Luxi Qiao (L)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

Emily Fisher (E)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

Lindsay McMurray (L)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

Selena Milicevic Sephton (S)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.
ORCID: 0000-0002-1105-6726

Matthew Hird (M)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

Nisha Kuzhuppilly-Ramakrishnan (N)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

David J Williamson (DJ)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

Xiouyun Zhou (X)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

Eryn Werry (E)

School of Chemistry, The University of Sydney, Building F11, Eastern Avenue, Sydney, NSW, 2006, Australia.

Michael Kassiou (M)

School of Chemistry, The University of Sydney, Building F11, Eastern Avenue, Sydney, NSW, 2006, Australia.

Saijinder Luthra (S)

GE Healthcare, Amersham, HP7 9LL, UK.

William Trigg (W)

GE Healthcare, Amersham, HP7 9LL, UK.

Franklin I Aigbirhio (FI)

Molecular Imaging Chemical Laboratory, Wolfson Brain Imaging Centre, Department of Clinical Neurosciences, University of Cambridge, Biomedical Campus, Cambridge, CB2 0SZ, UK.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Produits chimiques inorganiques › Isotopes › Radio-isotopes › Radio-isotopes du fluor › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Phénomènes génétiques › Variation génétique › Polymorphisme génétique › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Diagnostic › Techniques et procédures diagnostiques › Techniques de diagnostic radioisotopique › Scintigraphie › Tomoscintigraphie › Tomographie par émission de positons › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Disciplines des sciences naturelles › Science › Recherche › Étude de validation de principe › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Indicateurs et réactifs › Radiopharmaceutiques › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs GABA › Radiosynthesis of (R,S)-[
questionsmedicales.fr › Phénomènes chimiques › Phénomènes de chimie organique › Isomérie › Stéréoisomérie › Radiosynthesis of (R,S)-[