A5055131918- Radiopharmaceutical Chemistry and Applications
- Medical Imaging Techniques and Applications
- Neuroscience and Neuropharmacology Research
- Alzheimer's disease research and treatments
- Neurotransmitter Receptor Influence on Behavior
- Receptor Mechanisms and Signaling
- Lanthanide and Transition Metal Complexes
- Cancer, Hypoxia, and Metabolism
- Prostate Cancer Treatment and Research
- Amino Acid Enzymes and Metabolism
- Peptidase Inhibition and Analysis
- Computational Drug Discovery Methods
- Advanced MRI Techniques and Applications
- Chemical Synthesis and Analysis
- Medical Imaging and Pathology Studies
- Parkinson's Disease Mechanisms and Treatments
- Chemical Reactions and Isotopes
- Pharmacological Receptor Mechanisms and Effects
- Neurological disorders and treatments
- Dementia and Cognitive Impairment Research
- Ion channel regulation and function
- Glioma Diagnosis and Treatment
- S100 Proteins and Annexins
- Click Chemistry and Applications
- Virus-based gene therapy research
University of Pennsylvania
2016-2025
Capital Medical University
2016-2021
Chinese Institute for Brain Research
2015-2021
California University of Pennsylvania
2014-2021
Peking Union Medical College Hospital
2021
Beijing Normal University
2009-2021
Chinese Academy of Medical Sciences & Peking Union Medical College
2021
Centre for Movement Disorders
2020
Philadelphia University
1988-2014
Syracuse University
2008
To investigate the contribution of individual serotonin (5-hydroxytryptamine; 5-HT) receptors to mood control, we have used homologous recombination generate mice lacking specific serotonergic receptor subtypes. In present report, demonstrate that without 5-HT1A display decreased exploratory activity and increased fear aversive environments (open or elevated spaces). knockout also exhibited a immobility in forced swim test, an effect commonly associated with antidepressant treatment....
We studied the effects of low-frequency transcranial magnetic stimulation (TMS) on motor cortex excitability in humans. TMS at 0.1 Hz for 1 hour did not change cortical excitability. Stimulation 0.9 15 minutes (810 pulses), similar to parameters used induce long-term depression (LTD) slice preparations and vivo animal studies, led a mean decrease evoked potential (MEP) amplitude 19.5%. The lasted least after end stimulation. mechanism underlying this may be LTD. TMS-induced reduction has...
beta-amyloid plaques (Abeta plaques) in the brain, containing predominantly fibrillary Abeta peptide aggregates, represent a defining pathologic feature of Alzheimer disease (AD). Imaging agents targeting living human brain are potentially valuable as biomarkers pathogenesis processes AD. (E)-4-(2-(6-(2-(2-(2-(18)F-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methyl benzenamine ((18)F-AV-45) is such an agent currently phase III clinical studies for PET brain.In vitro binding (18)F-AV-45...
Glutamine-based PET imaging takes advantage of gliomas’ glutamine addiction and can be used to assess metabolic nutrient uptake in gliomas.
Radioactive prostate-specific membrane antigen (PSMA)-targeting agents are clinically useful for the diagnosis and treatment of patients with PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). Neuroendocrine-differentiated (NEPC), a highly aggressive subtype that is strongly associated poor clinical prognosis, may present reduced PSMA expression evade detection PSMA-targeted agents. Several studies have shown elevated uptake somatostatin receptor 2 (SSTR2) ligands in...
The competition between endogenous transmitters and radiolabeled ligands for in vivo binding to neuroreceptors might provide a method measure transmitter release the living human brain with noninvasive techniques such as positron emission tomography (PET) or single photon computerized (SPECT). In this study, we validated of amphetamine-induced dopamine SPECT nonhuman primates. Microdialysis experiments were conducted establish dose-response curve document how pretreatment depleter...
Abstract Several small molecule ligands for amyloid‐β (Aβ) fibrils deposited in brain have been developed to facilitate radiological diagnosis of Alzheimer’s disease (AD). Recently, the build‐up Aβ oligomers (AβO) has recognized as an additional hallmark AD and may play a more significant role early stages. Evidence suggests that quantitative assessment AβO would provide accurate index therapeutic effect drug trials. Therefore, there is urgent need develop methods efficient identification...
Strategies for treating Alzheimer's disease (AD) include therapies designed to decrease senile plaque (SP) formation and/or promote clearance of SPs, but clinical trials these treatments are limited by the lack effective methods monitor changes in burden brains living AD patients. However, because SPs extracellular deposits amyloid-β peptides (Aβ), it may be possible eventually develop radioligands that cross blood–brain barrier (BBB) and label so they can visualized current imaging methods....
A series of novel β-amyloid (Aβ) aggregate-specific ligands, 2-(4'-dimethylaminophenyl)-6-iodoimidazo[1,2-a]pyridine, 16(IMPY), and its related derivatives were prepared. An in vitro binding study with preformed Aβ aggregates showed that 16(IMPY) bromo derivative competed 2-(4'-dimethylaminophenyl)-6-iodobenzothiazole, [125I]7(TZDM), a known ligand for aggregates, high affinities (Ki = 15 10 nM, respectively). In autoradiography brain sections transgenic mouse (Tg2576) [125I]16(IMPY)...
We report for the first time that small molecule-based radiodiodinated ligands, showing selective binding to Aβ aggregates, cross intact blood−brain barrier by simple diffusion. Four novel ligands preferential labeling of amyloid aggregates Aβ(1−40) and Aβ(1−42) peptides, commonly associated with plaques in brain people Alzheimer's disease (AD), were developed. Two 125I-labeled styrylbenzenes, (E,E)-1-iodo-2,5-bis(3-hydroxycarbonyl-4-hydroxy)styrylbenzene, 12 (ISB),...
Identifying the factors contributing to etiology of anxiety and depression is critical for development more efficacious therapies. Serotonin (5-HT) intimately linked both disorders. The inhibitory serotonin-1A (5-HT 1A ) receptor exists in two separate populations with distinct effects on serotonergic signaling: (1) an autoreceptor that limits 5-HT release throughout brain (2) a heteroreceptor mediates responses released 5-HT. Traditional pharmacologic transgenic strategies have not...
Changes in gene expression, metabolism, and energy requirements are hallmarks of cancer growth self-sufficiency. Upregulation the PI3K/Akt/mTor pathway tumor cells has been shown to stimulate aerobic glycolysis, which enabled <sup>18</sup>F-FDG PET imaging. However, millions scans conducted per year, a significant number malignant tumors PET–negative. Recent studies suggest that several may use glutamine as key nutrient for survival. As an alternative metabolic tracer tumors,...
A versatile synthetic route to prepare all four stereoisomeric 4-fluoro-glutamines was developed by exploiting a Passerini three-component reaction. The skeleton of 4-substituted glutamine derivatives efficiently constructed. Subsequent four-step reactions, highlighted "neutralized" TASF fluorination, provided the desired products with high yields and excellent optical purity. optically pure fluorine-18 labeled 4-fluoroglutamines were also successfully prepared using either 18-crown-6/KHCO3...
PET provides a noninvasive means to evaluate the functional integrity of presynaptic monoaminergic system in living human brain. <b>Methods:</b> In this study, novel <sup>18</sup>F-labeled tetrabenazine derivative, <sup>18</sup>F-(+)fluoropropyldihydrotetrabenazine (<sup>18</sup>F-AV-133), was used for assessment vesicular monoamine transporters type 2 (VMAT2) 17 Parkinson disease (PD) patients and 6 healthy controls. The binding potential (BP) <sup>18</sup>F-AV-133 calculated using Logan...
Purpose To assess the clinical safety, pharmacokinetics, and tumor imaging characteristics of fluorine 18-(2S,4R)-4-fluoroglutamine (FGln), a glutamine analog radiologic agent. Materials Methods This study was approved by institutional review board conducted under U.S. Food Drug Administration-approved Investigational New application in accordance with Helsinki Declaration Health Insurance Portability Accountability Act. All patients provided written informed consent. Between January 2013...