Sofie Celen
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View article: cGMP-compliant high-yield automated production of [18F]AlF-FAPI-74: optimization of quality control and evaluation of molar dose impact
cGMP-compliant high-yield automated production of [18F]AlF-FAPI-74: optimization of quality control and evaluation of molar dose impact Open
A robust, fully automated, and GMP-compliant production process for [18F]AlF-FAPI-74 is reported with high yield, purity, and stability, suitable for centralized production and distribution. The improved radio-HPLC method enhances quality …
View article: Radiosynthesis and Evaluation of [<sup>18</sup>F]FEHSP990 as Novel PET Tracer for Hsp90 PET Imaging
Radiosynthesis and Evaluation of [<sup>18</sup>F]FEHSP990 as Novel PET Tracer for Hsp90 PET Imaging Open
Heat shock protein 90 (Hsp90) is a critical chaperone in the protein quality control system, essential for maintaining cellular proteostasis. Aberrant Hsp90 function has been implicated in cancer and neurodegenerative disorders, making it …
View article: Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid <i>α</i>/<i>β</i>-Hydrolase Domain 6 (ABHD6)
Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid <i>α</i>/<i>β</i>-Hydrolase Domain 6 (ABHD6) Open
Multimodal imaging provides rich biological information, which can be exploited to study drug activity, disease associated phenotypes, and pharmacological responses. Here we show discovery and validation of a new probe targeting the endoca…
View article: Translation of HDAC6 PET Imaging Using [<sup>18</sup>F]EKZ-001–cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates
Translation of HDAC6 PET Imaging Using [<sup>18</sup>F]EKZ-001–cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates Open
Histone deacetylase 6 (HDAC6) is a multifunctional cytoplasmic enzyme involved in diverse cellular processes such as intracellular transport and protein quality control. Inhibition of HDAC6 can alleviate defects in cell and rodent models o…
View article: TSPO Versus P2X7 as a Target for Neuroinflammation: An In Vitro and In Vivo Study
TSPO Versus P2X7 as a Target for Neuroinflammation: An In Vitro and In Vivo Study Open
Neuroinflammation is important in amyotrophic lateral sclerosis (ALS). The P2X7 receptor (P2X7R) is a promising target for neuroinflammation. The objective of this study was to compare 18F-DPA714, a second-generation translocator protein t…
View article: Evaluation of [<sup>11</sup>C]NMS-E973 as a PET tracer for <i>in vivo</i> visualisation of HSP90
Evaluation of [<sup>11</sup>C]NMS-E973 as a PET tracer for <i>in vivo</i> visualisation of HSP90 Open
Heat shock protein 90 is an ATP-dependent molecular chaperone important for folding, maturation and clearance of aberrantly expressed proteins and is abundantly expressed (1-2% of all proteins) in the cytosol of all normal cells. In some t…
View article: Preclinical evaluation of [<sup>18</sup>F]MA3: a CB<sub>2</sub> receptor agonist radiotracer for PET
Preclinical evaluation of [<sup>18</sup>F]MA3: a CB<sub>2</sub> receptor agonist radiotracer for PET Open
Background and Purpose Non‐invasive in vivo imaging of cannabinoid CB 2 receptors using PET is pursued to study neuroinflammation. The purpose of this study is to evaluate the in vivo binding specificity of [ 18 F]MA3, a CB 2 receptor agon…
View article: Brain Imaging of Alzheimer Dementia Patients and Elderly Controls with <sup>18</sup>F-MK-6240, a PET Tracer Targeting Neurofibrillary Tangles
Brain Imaging of Alzheimer Dementia Patients and Elderly Controls with <sup>18</sup>F-MK-6240, a PET Tracer Targeting Neurofibrillary Tangles Open
18F-MK-6240 (18F-labeled 6-(fluoro)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine) is a highly selective, subnanomolar-affinity PET tracer for imaging neurofibrillary tangles (NFTs). Plasma kinetics, brain uptake, and preliminary qu…
View article: Fatty Acid Amide Hydrolase Inhibition by JNJ‐42165279: A Multiple‐Ascending Dose and a Positron Emission Tomography Study in Healthy Volunteers
Fatty Acid Amide Hydrolase Inhibition by JNJ‐42165279: A Multiple‐Ascending Dose and a Positron Emission Tomography Study in Healthy Volunteers Open
Inhibition of fatty acid amide hydrolase (FAAH) potentiates endocannabinoid activity and is hypothesized to have therapeutic potential for mood and anxiety disorders and pain. The clinical profile of JNJ‐42165279, an oral selective FAAH in…
View article: [P3–381]: FIRST EVALUATION OF THE NEUROFIBRILLARY TANGLES RADIOLIGAND [<sup>18</sup>F]MK‐6240 IN ALZHEIMER's DISEASE PATIENTS
[P3–381]: FIRST EVALUATION OF THE NEUROFIBRILLARY TANGLES RADIOLIGAND [<sup>18</sup>F]MK‐6240 IN ALZHEIMER's DISEASE PATIENTS Open
Dementia correlates strongly with the extent of neurofibrillary tangles (NFT). We recently disclosed [18F]MK-6240, a potent and selective NFT radioligand designed to be more specific and sensitive than previously known NFT PET radioligands…
View article: [IC‐P‐177]: FIRST EVALUATION OF THE NEUROFIBRILLARY TANGLES RADIOLIGAND [<sup>18</sup>F]MK‐6240 IN ALZHEIMER's DISEASE PATIENTS
[IC‐P‐177]: FIRST EVALUATION OF THE NEUROFIBRILLARY TANGLES RADIOLIGAND [<sup>18</sup>F]MK‐6240 IN ALZHEIMER's DISEASE PATIENTS Open
Dementia correlates strongly with the extent of neurofibrillary tangles (NFT). We recently disclosed [18F]MK-6240, a potent and selective NFT radioligand designed to be more specific and sensitive than previously known NFT PET radioligands…
View article: [18F]<scp>JNJ</scp>42259152 binding to phosphodiesterase 10A, a key regulator of medium spiny neuron excitability, is altered in the presence of cyclic <scp>AMP</scp>
[18F]<span>JNJ</span>42259152 binding to phosphodiesterase 10A, a key regulator of medium spiny neuron excitability, is altered in the presence of cyclic <span>AMP</span> Open
Phosphodiesterase 10A ( PDE 10A) is a key regulator of medium spiny neuron excitability. Therefore, it plays an important role in the regulation of motor, reward, and cognitive processes. Despite the interest in PDE 10A as a drug and posit…
View article: What We Observe In Vivo Is Not Always What We See In Vitro: Development and Validation of <sup>11</sup>C-JNJ-42491293, A Novel Radioligand for mGluR2
What We Observe In Vivo Is Not Always What We See In Vitro: Development and Validation of <sup>11</sup>C-JNJ-42491293, A Novel Radioligand for mGluR2 Open
On the basis of in vivo selectivity issues suggested by human distribution and demonstrated in knockout rat models, 11C-JNJ-42491293 was considered unsuitable as a specific PET ligand for in vivo imaging of mGluR2. These results emphasize …
View article: Preclinical Evaluation of a P2X7 Receptor–Selective Radiotracer: PET Studies in a Rat Model with Local Overexpression of the Human P2X7 Receptor and in Nonhuman Primates
Preclinical Evaluation of a P2X7 Receptor–Selective Radiotracer: PET Studies in a Rat Model with Local Overexpression of the Human P2X7 Receptor and in Nonhuman Primates Open
JNJ-54173717 is a high-affinity P2X7R antagonist. An animal rat model stably expressing hP2X7R was developed and validated, identifying favorable characteristics for (11)C-JNJ-54173717 as a PET radioligand for in vivo visualization of hP2X…
View article: Comparison of New Tau PET-Tracer Candidates With [<sup>18</sup>F]T808 and [<sup>18</sup>F]T807
Comparison of New Tau PET-Tracer Candidates With [<sup>18</sup>F]T808 and [<sup>18</sup>F]T807 Open
Early clinical results of two tau tracers, [ 18 F]T808 and [ 18 F]T807, have recently been reported. In the present study, the biodistribution, radiometabolite quantification, and competition-binding studies were performed in order to acqu…