Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising 18F-Labeled Ligand

Translation of 11C-labeled tracer synthesis to a CGMP environment as exemplified by [11C]ER176 for PET imaging of human TSPO

(2021) Jinsoo Hong et al.   Nature Protocols

Synthesis of [18 F]Fluoroform with High Molar Activity

(2020) Anna Pees et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Rapid and Efficient Synthesis of [11C]Trifluoromethylarenes from Primary Aromatic Amines and [11C]CuCF3

(2020) Nicholas J. Young et al.   ACS Omega

A Gas Phase Route to [18F]fluoroform with Limited Molar Activity Dilution

(2019) Bo Yeun Yang et al.   Scientific Reports

Hypervalent aryliodine compounds as precursors for radiofluorination

(2018) Victor W. Pike   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Comparison of four 11C-labeled PET ligands to quantify translocator protein 18 kDa (TSPO) in human brain: (R)-PK11195, PBR28, DPA-713, and ER176—based on recent publications that measured specific-to-non-displaceable ratios

(2017) Masahiro Fujita et al.   EJNMMI Research

Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging

(2016) Victor W. Pike   CURRENT MEDICINAL CHEMISTRY

11 C-ER176, a Radioligand for 18-kDa Translocator Protein, Has Adequate Sensitivity to Robustly Image All Three Affinity Genotypes in Human Brain

(2016) Masamichi Ikawa et al.   JOURNAL OF NUCLEAR MEDICINE

TSPO ligand residence time: a new parameter to predict compound neurosteroidogenic efficacy

(2016) Barbara Costa et al.   Scientific Reports

Synthesis and Evaluation of Translocator 18 kDa Protein (TSPO) Positron Emission Tomography (PET) Radioligands with Low Binding Sensitivity to Human Single Nucleotide Polymorphism rs6971

(2014) Paolo Zanotti-Fregonara et al.   ACS Chemical Neuroscience

A Universal Procedure for the [18F]Trifluoromethylation of Aryl Iodides and Aryl Boronic Acids with Highly Improved Specific Activity

(2014) Dion van der Born et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

TSPO ligand residence time influences human glioblastoma multiforme cell death/life balance

(2014) Barbara Costa et al.   APOPTOSIS

[18F]CuCF3: A [18F]Trifluoromethylating Agent for Arylboronic Acids and Aryl Iodides

(2014) Pavel Ivashkin et al.   CHEMISTRY-A EUROPEAN JOURNAL

Structure–Activity Relationship Refinement and Further Assessment of 4-Phenylquinazoline-2-carboxamide Translocator Protein Ligands as Antiproliferative Agents in Human Glioblastoma Tumors

(2014) Sabrina Castellano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Copper-Catalyzed [18F]Fluorination of (Mesityl)(aryl)iodonium Salts

(2014) Naoko Ichiishi et al.   ORGANIC LETTERS

One-Pot Synthesis and Applications of N-Heteroaryl Iodonium Salts

(2014) Marcin Bielawski et al.   ChemistryOpen

Setting expectations in molecular optimizations: Strengths and limitations of commonly used composite parameters

(2013) Michael D. Shultz   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Quantification of the Specific Translocator Protein Signal of 18F-PBR111 in Healthy Humans: A Genetic Polymorphism Effect on In Vivo Binding

(2013) Q. Guo et al.   JOURNAL OF NUCLEAR MEDICINE

A broadly applicable [18F]trifluoromethylation of aryl and heteroaryl iodides for PET imaging

(2013) Mickael Huiban et al.   Nature Chemistry

Solution Structures of the Prototypical 18 kDa Translocator Protein Ligand, PK 11195, Elucidated with 1H/13C NMR Spectroscopy and Quantum Chemistry

(2012) Yong-Sok Lee et al.   ACS Chemical Neuroscience

A Genetic Polymorphism for Translocator Protein 18 Kda Affects both in Vitro and in Vivo Radioligand Binding in Human Brain to this Putative Biomarker of Neuroinflammation

(2012) William C Kreisl et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Translocator Protein (18 kDa) Polymorphism (rs6971) Explains in-vivo Brain Binding Affinity of the PET Radioligand [18F]-FEPPA

(2012) Romina Mizrahi et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Synthesis and Biological Evaluation of 4-Phenylquinazoline-2-carboxamides Designed as a Novel Class of Potent Ligands of the Translocator Protein

(2012) Sabrina Castellano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Weinreb Amidation as the Cornerstone of an Improved Synthetic Route to A-Ring-Modified Derivatives of Luotonin A

(2012) Norbert Haider et al.   MOLECULES

An 18-kDa Translocator Protein (TSPO) Polymorphism Explains Differences in Binding Affinity of the PET Radioligand PBR28

(2011) David R Owen et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

PET tracers for the peripheral benzodiazepine receptor and uses thereof

(2010) Pernilla J. Schweitzer et al.   DRUG DISCOVERY TODAY

Two Binding Sites for [3H]PBR28 in Human Brain: Implications for TSPO PET Imaging of Neuroinflammation

(2010) David R Owen et al.   JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM

Mixed-Affinity Binding in Humans with 18-kDa Translocator Protein Ligands

(2010) D. R. J. Owen et al.   JOURNAL OF NUCLEAR MEDICINE

Cholesterol transport in steroid biosynthesis: Role of protein–protein interactions and implications in disease states

(2009) Malena B. Rone et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Radiolabelled Molecules for Imaging the Translocator Protein (18 kDa) Using Positron Emission Tomography

(2009) Frederic Dolle et al.   CURRENT MEDICINAL CHEMISTRY

Single-Step High-Yield Radiosynthesis and Evaluation of a Sensitive18F-Labeled Ligand for Imaging Brain Peripheral Benzodiazepine Receptors with PET

(2009) Emmanuelle Briard et al.   JOURNAL OF MEDICINAL CHEMISTRY

Initial Evaluation of 11C-DPA-713, a Novel TSPO PET Ligand, in Humans

(2009) C. J. Endres et al.   JOURNAL OF NUCLEAR MEDICINE

Comparison of [11C]-(R)-PK 11195 and [11C]PBR28, two radioligands for translocator protein (18 kDa) in human and monkey: Implications for positron emission tomographic imaging of this inflammation biomarker

(2009) William C. Kreisl et al.   NEUROIMAGE

Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers

(2008) Fabien Chauveau et al.   EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING

Chemistry with [18F]Fluoride Ion

(2008) Lisheng Cai et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Pd-Catalyzed Direct Arylation of Tautomerizable Heterocycles with Aryl Boronic Acids via C−OH Bond Activation Using Phosphonium Salts

(2008) Fu-An Kang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Radiosynthesis and initial evaluation of [18F]-FEPPA for PET imaging of peripheral benzodiazepine receptors

(2008) Alan A. Wilson et al.   NUCLEAR MEDICINE AND BIOLOGY

Synthesis and Evaluation in Monkey of Two Sensitive11C-Labeled Aryloxyanilide Ligands for Imaging Brain Peripheral Benzodiazepine Receptors In Vivo

(2007) Emmanuelle Briard et al.   JOURNAL OF MEDICINAL CHEMISTRY

Brain and whole-body imaging in nonhuman primates of [11C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptors

(2007) Masao Imaizumi et al.   NEUROIMAGE

Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation

(2007) Masahiro Fujita et al.   NEUROIMAGE