Jeih‐San Liow
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View article: [11C]Fentanyl: radiosynthesis and preclinical pet imaging for its pharmacokinetics
[11C]Fentanyl: radiosynthesis and preclinical pet imaging for its pharmacokinetics Open
Background Fentanyl is a potent synthetic opioid widely used for pain management and anesthesia, but the high prevalence of its misuse and its key contribution to overdose fatalities in the United States have made it a major drug of concer…
View article: [11C]Fentanyl: Radiosynthesis and Preclinical PET Imaging for Its Pharmacokinetics
[11C]Fentanyl: Radiosynthesis and Preclinical PET Imaging for Its Pharmacokinetics Open
View article: Evaluation of [18F]fluoroestradiol and ChRERα as a gene expression PET reporter system in rhesus monkey brain
Evaluation of [18F]fluoroestradiol and ChRERα as a gene expression PET reporter system in rhesus monkey brain Open
View article: Robust Quantification of Phosphodiesterase-4D in Monkey Brain with PET and<sup>11</sup>C-Labeled Radioligands That Avoid Radiometabolite Contamination
Robust Quantification of Phosphodiesterase-4D in Monkey Brain with PET and<sup>11</sup>C-Labeled Radioligands That Avoid Radiometabolite Contamination Open
Phosphodiesterase-4D (PDE4D) has emerged as a significant target for treating neuropsychiatric disorders, but no PET radioligand currently exists for robustly quantifying human brain PDE4D to assist biomedical research and drug discovery. …
View article: Synthesis and preclinical evaluation of [11C]uPSEM792 for PSAM4-GlyR based chemogenetics
Synthesis and preclinical evaluation of [11C]uPSEM792 for PSAM4-GlyR based chemogenetics Open
View article: <b>Evaluation of [</b><sup><strong>18</strong></sup><b>F]fluoroestradiol and ChRERα </b><b>as a gene expression PET reporter system </b><b>in rhesus monkey brain</b>
<b>Evaluation of [</b><sup><strong>18</strong></sup><b>F]fluoroestradiol and ChRERα </b><b>as a gene expression PET reporter system </b><b>in rhesus monkey brain</b> Open
Positron emission tomography (PET) reporter systems are a valuable means of estimating the level of expression of a transgene in vivo. For example, the safety and efficacy of gene therapy approaches to the treatment of neurological …
View article: In vivo evaluation of a novel 18F-labeled PET radioligand for translocator protein 18 kDa (TSPO) in monkey brain
In vivo evaluation of a novel 18F-labeled PET radioligand for translocator protein 18 kDa (TSPO) in monkey brain Open
Purpose [ 18 F]SF51 was previously found to have high binding affinity and selectivity for 18 kDa translocator protein (TSPO) in mouse brain. This study sought to assess the ability of [ 18 F]SF51 to quantify TSPO in rhesus monkey brain. M…
View article: Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors
Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors Open
View article: Discovery of a High-Affinity Fluoromethyl Analog of [<sup>11</sup>C]5-Cyano-<i>N</i>-(4-(4-methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide ([<sup>11</sup>C]CPPC) and Their Comparison in Mouse and Monkey as Colony-Stimulating Factor 1 Receptor Positron Emission Tomography Radioligands
Discovery of a High-Affinity Fluoromethyl Analog of [<sup>11</sup>C]5-Cyano-<i>N</i>-(4-(4-methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide ([<sup>11</sup>C]CPPC) and Their Comparison in Mouse and Monkey as Colony-Stimulating Factor 1 Receptor Positron Emission Tomography Radioligands Open
[11C]CPPC has been advocated as a radioligand for colony-stimulating factor 1 receptor (CSF1R) with the potential for imaging neuroinflammation in human subjects with positron emission tomography (PET). This study sought …
View article: Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors
Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors Open
We recently reported 11C-NR2B-SMe ([S-methyl-11C](R,S)-7-thiomethoxy-3-(4-(4-methyl-phenyl)butyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepin-1-ol) and its enantiomers as candidate radioligands for imaging the GluN2B subunit…
View article: In vivo evaluation of a novel 18F-labeled PET radioligand for translocator protein 18kDa (TSPO) in monkey brain
In vivo evaluation of a novel 18F-labeled PET radioligand for translocator protein 18kDa (TSPO) in monkey brain Open
Purpose: 18F-SF51 was previously found to have high binding affinity and selectivity for 18kDa translocator protein (TSPO) in mouse brain. This study sought to further evaluate the suitability of 18F-SF51 for absolute…
View article: Whole-Body PET Imaging in Humans Shows That<sup>11</sup>C-PS13 Is Selective for Cyclooxygenase-1 and Can Measure the In Vivo Potency of Nonsteroidal Antiinflammatory Drugs
Whole-Body PET Imaging in Humans Shows That<sup>11</sup>C-PS13 Is Selective for Cyclooxygenase-1 and Can Measure the In Vivo Potency of Nonsteroidal Antiinflammatory Drugs Open
Both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) convert arachidonic acid to prostaglandin H2, which has proinflammatory effects. The recently developed PET radioligand 11C-PS13 has excellent in vivo selecti…
View article: First-in-Human Evaluation of<sup>18</sup>F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B
First-in-Human Evaluation of<sup>18</sup>F-PF-06445974, a PET Radioligand That Preferentially Labels Phosphodiesterase-4B Open
Phosphodiesterase-4 (PDE4), which metabolizes the second messenger cyclic adenosine monophosphate (cAMP), has 4 isozymes: PDE4A, PDE4B, PDE4C, and PDE4D. PDE4B and PDE4D have the highest expression in the brain and may play a role in the p…
View article: Naloxone’s dose-dependent displacement of [11C]carfentanil and duration of receptor occupancy in the rat brain
Naloxone’s dose-dependent displacement of [11C]carfentanil and duration of receptor occupancy in the rat brain Open
View article: Naloxone’s displacement of [11C]carfentanil and duration of receptor occupancy in the rat brain: implications for opioid overdose reversal
Naloxone’s displacement of [11C]carfentanil and duration of receptor occupancy in the rat brain: implications for opioid overdose reversal Open
The continuous rise in opioid overdoses in the United States is predominantly driven by very potent synthetic opioids, mostly fentanyl and its derivatives (fentanyls). Although naloxone (NLX) has been shown to effectively reverse overdoses…
View article: In Vivo Evaluation of 6 Analogs of <sup>11</sup>C-ER176 as Candidate <sup>18</sup>F-Labeled Radioligands for 18-kDa Translocator Protein
In Vivo Evaluation of 6 Analogs of <sup>11</sup>C-ER176 as Candidate <sup>18</sup>F-Labeled Radioligands for 18-kDa Translocator Protein Open
Because of its excellent ratio of specific to nondisplaceable uptake, the radioligand 11C-ER176 can successfully image 18-kDa translocator protein (TSPO), a biomarker of inflammation, in the human brain and accurately quantify t…
View article: Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising <sup>18</sup>F-Labeled Ligand
Synthesis and Screening in Mice of Fluorine-Containing PET Radioligands for TSPO: Discovery of a Promising <sup>18</sup>F-Labeled Ligand Open
Translocator protein 18 kDa (TSPO) is a biomarker of neuroinflammation. [11C]ER176 robustly quantifies TSPO in the human brain with positron emission tomography (PET), irrespective of subject genotype. We aimed to develop an ER1…
View article: [<sup>11</sup>C]deschloroclozapine is an improved PET radioligand for quantifying a human muscarinic DREADD expressed in monkey brain
[<sup>11</sup>C]deschloroclozapine is an improved PET radioligand for quantifying a human muscarinic DREADD expressed in monkey brain Open
Previous work found that [ 11 C]deschloroclozapine ([ 11 C]DCZ) is superior to [ 11 C]clozapine ([ 11 C]CLZ) for imaging Designer Receptors Exclusively Activated by Designer Drugs (DREADDs). This study used PET to quantitatively and separa…
View article: Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB<sub>1</sub>R) Antagonist
Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB<sub>1</sub>R) Antagonist Open
Seven-transmembrane receptors signal via G-protein- and β-arrestin-dependent pathways. We describe a peripheral CB1R antagonist (MRI-1891) highly biased toward inhibiting CB1R-induced β-arrestin-2 (βArr2) recruitment …
View article: Region- and voxel-based quantification in human brain of [18F]LSN3316612, a radioligand for O-GlcNAcase
Region- and voxel-based quantification in human brain of [18F]LSN3316612, a radioligand for O-GlcNAcase Open
View article: Synthesis of [<sup>18</sup>F]PS13 and Evaluation as a PET Radioligand for Cyclooxygenase-1 in Monkey
Synthesis of [<sup>18</sup>F]PS13 and Evaluation as a PET Radioligand for Cyclooxygenase-1 in Monkey Open
Cyclooxygenase-1 (COX-1) and its isozyme COX-2 are key enzymes in the syntheses of prostanoids. Imaging of COX-1 and COX-2 selective radioligands with positron emission tomography (PET) may clarify how these enzymes are involved in inflamm…
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: PET quantification of brain O-GlcNAcase with [18F]LSN3316612 in healthy human volunteers
PET quantification of brain O-GlcNAcase with [18F]LSN3316612 in healthy human volunteers Open
View article: Evaluation of <sup>11</sup>C-NR2B-SMe and Its Enantiomers as PET Radioligands for Imaging the NR2B Subunit Within the NMDA Receptor Complex in Rats
Evaluation of <sup>11</sup>C-NR2B-SMe and Its Enantiomers as PET Radioligands for Imaging the NR2B Subunit Within the NMDA Receptor Complex in Rats Open
[S-methyl-11C](±)-7-methoxy-3-(4-(4-(methylthio)phenyl)butyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepin-1-ol (11C-NR2B-SMe) and its enantiomers were synthesized as candidates for imaging the NR2…
View article: Neuroinflammation in neocortical epilepsy measured by PET imaging of translocator protein
Neuroinflammation in neocortical epilepsy measured by PET imaging of translocator protein Open
Objectives Neuroinflammation, implicated in epilepsy, can be imaged in humans with positron emission tomography (PET) ligands for translocator protein 18 kDa (TSPO). Previous studies in patients with temporal lobe epilepsy and mesial tempo…
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: The Evaluation of Dynamic FDG-PET for Detecting Epileptic Foci and Analyzing Reduced Glucose Phosphorylation in Refractory Epilepsy
The Evaluation of Dynamic FDG-PET for Detecting Epileptic Foci and Analyzing Reduced Glucose Phosphorylation in Refractory Epilepsy Open
Aims: Static fluorodeoxyglucose (FDG)-positron emission tomographic (PET) imaging plays an important role in the localization of epileptic foci. Dynamic FDG PET allows calculation of kinetic parameters. The aim of this study was to …
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: Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys
Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys Open
This study assessed whether the newly developed PET radioligands 11C-PS13 and 11C-MC1 could image constitutive levels of cyclooxygenase (COX)-1 and COX-2, respectively, in rhesus monkeys. Methods: After intrave…
View article: 3-Substituted 1,5-Diaryl-1<i>H</i>-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 2: Selection and Evaluation of [<sup>11</sup>C]PS13 for Quantitative Imaging
3-Substituted 1,5-Diaryl-1<i>H</i>-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 2: Selection and Evaluation of [<sup>11</sup>C]PS13 for Quantitative Imaging Open
In our preceding paper (Part 1), we identified three 1,5-bis-diaryl-1,2,4-triazole-based compounds that merited evaluation as potential positron emission tomography (PET) radioligands for selectively imaging cyclooxygenase-1 (COX-1) in mon…