Shuiyu Lu
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View article: Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes
Expanding tracer space for positron emission tomography with high molar activity 18F-labeled α,α-difluoromethylalkanes Open
View article: Gas Phase Transformations in Carbon-11 Chemistry
Gas Phase Transformations in Carbon-11 Chemistry Open
The short-lived positron-emitter carbon-11 (t1/2 = 20.4 min; β+, 99.8%) is prominent for labeling tracers for use in biomedical research with positron emission tomography (PET). Carbon-11 is produced for this purpose with a cyclotron, nowa…
View article: Gas Phase Transformations in Carbon-11 Chemistry
Gas Phase Transformations in Carbon-11 Chemistry Open
The short-lived positron-emitter carbon-11 (t1/2 = 20.4 min; b+, 99.8%) is prominent for labeling tracers for use in biomedical research with positron emission tomography (PET). Carbon-11 is produced for this purpose with a cyclotron, nowa…
View article: On the Risk of <sup>18</sup>F-Regioisomer Formation in the Copper-Free Radiofluorination of Aryliodonium Precursors
On the Risk of <sup>18</sup>F-Regioisomer Formation in the Copper-Free Radiofluorination of Aryliodonium Precursors Open
Aryliodonium precursors are widely applied for copper-free labeling of positron emission tomography (PET) tracers with fluorine-18. We assessed 18F-fluoroarene regioisomer formation in examples of these labeling methods. Aryliod…
View article: An Empirical Quantitative Structure-Activity Relationship Equation Assists the Discovery of High-Affinity Phosphodiesterase 4D Inhibitors as Leads to PET Radioligands
An Empirical Quantitative Structure-Activity Relationship Equation Assists the Discovery of High-Affinity Phosphodiesterase 4D Inhibitors as Leads to PET Radioligands Open
A positron emission tomography (PET) radioligand for imaging phosphodiesterase 4D (PDE4D) would benefit drug discovery and the investigation of neuropsychiatric disorders. The most promising radioligand to date, namely, [11C]T16…
View article: Broad Scope and High‐Yield Access to Unsymmetrical Acyclic [<sup>11</sup>C]Ureas for Biomedical Imaging from [<sup>11</sup>C]Carbonyl Difluoride
Broad Scope and High‐Yield Access to Unsymmetrical Acyclic [<sup>11</sup>C]Ureas for Biomedical Imaging from [<sup>11</sup>C]Carbonyl Difluoride Open
Effective methods are needed for labelling acyclic ureas with carbon‐11 ( t 1/2 =20.4 min) as potential radiotracers for biomedical imaging with positron emission tomography (PET). Herein, we describe the rapid and high‐yield syntheses of …
View article: PET ligands [ <sup>18</sup> F]LSN3316612 and [ <sup>11</sup> C]LSN3316612 quantify <i>O</i> -linked-β- <i>N</i> -acetyl-glucosamine hydrolase in the brain
PET ligands [ <sup>18</sup> F]LSN3316612 and [ <sup>11</sup> C]LSN3316612 quantify <i>O</i> -linked-β- <i>N</i> -acetyl-glucosamine hydrolase in the brain Open
Two radioligands, [ 18 F]LSN3316612 and [ 11 C]LSN3316612, image and quantify brain O -linked-β- N -acetyl-glucosamine hydrolase in vivo.
View article: [<sup>11</sup>C]Carbonyl Difluoride—a New and Highly Efficient [<sup>11</sup>C]Carbonyl Group Transfer Agent
[<sup>11</sup>C]Carbonyl Difluoride—a New and Highly Efficient [<sup>11</sup>C]Carbonyl Group Transfer Agent Open
Herein, the synthesis and use of [ 11 C]carbonyl difluoride for labeling heterocycles with [ 11 C]carbonyl groups in high molar activity is described. A very mild single‐pass gas‐phase conversion of [ 11 C]carbon monoxide into [ 11 C]carbo…
View article: Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors
Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors Open
View article: [O-methyl-11C]N-(4-(4-(3-Chloro-2-methoxyphenyl)-piperazin-1-yl)butyl)-1H-indole-2-carboxamide ([11C]BAK4-51) Is an Efflux Transporter Substrate and Ineffective for PET Imaging of Brain D3 Receptors in Rodents and Monkey
[O-methyl-11C]N-(4-(4-(3-Chloro-2-methoxyphenyl)-piperazin-1-yl)butyl)-1H-indole-2-carboxamide ([11C]BAK4-51) Is an Efflux Transporter Substrate and Ineffective for PET Imaging of Brain D3 Receptors in Rodents and Monkey Open
Selective high-affinity antagonists for the dopamine D3 receptor (D3R) are sought for treating substance use disorders. Positron emission tomography (PET) with an effective D3R radioligand could be a useful tool for the development of such…
View article: Front Cover: [<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography (ChemMedChem 2/2018)
Front Cover: [<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography (ChemMedChem 2/2018) Open
The Front Cover shows the in vivo evaluation of a prospective radioligand for cPLA2a, a biomarker for neuroinflammation, in a mouse brain by positron emission tomography (PET). In order to reversibly bind to the enzyme target, the 11C-labe…
View article: [<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography
[<i>Carboxyl</i>‐<sup>11</sup>C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography Open
Cytosolic phospholipase A2α (cPLA2α) may play a critical role in neuropsychiatric and neurodegenerative disorders associated with oxidative stress and neuroinflammation. An effective PET radioligand for imaging cPLA2α in living brain might…
View article: Quinuclidine and DABCO Enhance the Radiofluorination of 5‐Substituted 2‐Halopyridines
Quinuclidine and DABCO Enhance the Radiofluorination of 5‐Substituted 2‐Halopyridines Open
Positron emission tomography (PET) is an important molecular imaging technique for medical diagnosis, biomedical research and drug development. PET tracers for molecular imaging contain β + ‐emitting radionuclides, such as carbon‐11 ( t 1/…
View article: 11C-Labeling of Aryl Ketones as Candidate Histamine Subtype-3 Receptor PET Radioligands through Pd(0)-Mediated 11C-Carbonylative Coupling
11C-Labeling of Aryl Ketones as Candidate Histamine Subtype-3 Receptor PET Radioligands through Pd(0)-Mediated 11C-Carbonylative Coupling Open
Pd(0)-mediated coupling between iodoarenes, [11C]carbon monoxide and aryltributylstannanes has been used to prepare simple model [11C]aryl ketones. Here, we aimed to label four 2-aminoethylbenzofuran chemotype based molecules ([11C]1–4) in…
View article: Crown Ether Nucleophilic Catalysts (CENCs): Agents for Enhanced Silicon Radiofluorination
Crown Ether Nucleophilic Catalysts (CENCs): Agents for Enhanced Silicon Radiofluorination Open
New bifunctional phase transfer agents were synthesized and investigated for their abilities to promote rapid fluorination at silicon. These agents, dubbed crown ether nucleophilic catalysts (CENCs), are 18-crown-6 derivatives containing a…
View article: Correction to “An Investigation of (Diacetoxyiodo)arenes as Precursors for Preparing No-Carrier-Added [<sup>18</sup>F]Fluoroarenes from Cyclotron-Produced [<sup>18</sup>F]Fluoride Ion”
Correction to “An Investigation of (Diacetoxyiodo)arenes as Precursors for Preparing No-Carrier-Added [<sup>18</sup>F]Fluoroarenes from Cyclotron-Produced [<sup>18</sup>F]Fluoride Ion” Open
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to “An Investigation of (Diacetoxyiodo)arenes as Precursors for Preparing No-Carrier-Added [18F]Fluoroarenes from Cyclotron-Produ…
View article: [ carbonyl - 11 C]4-Fluoro- N -methyl- N -(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([ 11 C]FIMX) is an effective radioligand for PET imaging of metabotropic glutamate receptor 1 (mGluR1) in monkey brain
[ carbonyl - 11 C]4-Fluoro- N -methyl- N -(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([ 11 C]FIMX) is an effective radioligand for PET imaging of metabotropic glutamate receptor 1 (mGluR1) in monkey brain Open
View article: The Inhibitor Ko143 Is Not Specific for ABCG2
The Inhibitor Ko143 Is Not Specific for ABCG2 Open