A5101423838- Medical Imaging Techniques and Applications
- Pharmacological Receptor Mechanisms and Effects
- Cancer, Hypoxia, and Metabolism
- Chemical Reactions and Isotopes
- Radiopharmaceutical Chemistry and Applications
- Neuroscience and Neuropharmacology Research
- Receptor Mechanisms and Signaling
- Neuropeptides and Animal Physiology
- Fluorine in Organic Chemistry
- Virus-based gene therapy research
- Advanced biosensing and bioanalysis techniques
- Glioma Diagnosis and Treatment
- RNA Interference and Gene Delivery
- Enzyme function and inhibition
- Ion channel regulation and function
- Histone Deacetylase Inhibitors Research
- Hemoglobin structure and function
- bioluminescence and chemiluminescence research
- Cancer therapeutics and mechanisms
- Inflammatory mediators and NSAID effects
- Medical Imaging and Pathology Studies
- Polysaccharides and Plant Cell Walls
- Cancer-related Molecular Pathways
- Mesoporous Materials and Catalysis
- Epilepsy research and treatment
National Taiwan University Hospital
2015-2022
Tri-Service General Hospital
2018
University of Pennsylvania
1997-2004
Philadelphia University
2000
Creighton University
1992-1998
University of Nebraska Medical Center
1998
Brookhaven National Laboratory
1980-1997
Shanghai Medical College of Fudan University
1997
United States Department of Veterans Affairs
1997
Mount Sinai Hospital
1997
Abstract: The butyrophenone neuroleptics spiroperidol, benperidol, and haloperidol were radiolabeled with fluorine‐18 studied in baboon brain using positron emission transaxial tomography (PETT). Pretreatment of the a high pharmacological dose (+)‐butaclamol reduced specifically bound component radioactivity distribution striatum to approximately found cerebellum. Comparative studies kinetics over 4‐h period indicated that either [ 18 F]spiroperidol or F]benperidol may be suitable for...
Abstract A rapid synthesis of 2‐deoxy‐2‐fluoro‐D‐glucose (3) from xenon difluoride is described. Reaction 3,4,6‐tri‐O‐acetyl‐D‐glucal (1) with in ethyl ether the presence BF 3 ·OEt 2 for 20 minutes gave 2‐deoxy‐2‐fluoro‐ 3,4,6‐tri‐O‐acetyl‐D‐glucopyranosyl fluoride (2) 70‐80% chemical yield. Hydrolysis N HCl 50% overall yield a time 60 minutes. Preliminary results indicate that this method can be used to synthesize 2‐deoxy‐2‐ [ 18 F] fluoro‐D‐glucose.
No-carrier-added (NCA)[11C](±)-ketamine (2a) and its enantiomers (+)-2b (−)-2c were synthesized by methylation of the corresponding norketamine (1a-c) with [11C]H3I in an overall radiochemical yield 20% (EOB) specific activities 0.35–0.45 Ci/μmole at EOB a synthesis time 40 min from EOB. Compound 2a was metabolized rapidly mouse brain labeled metabolites appeared baboon plasma. PET studies compounds 2a–c showed that influx 2a-c into high for first few but radioactivity then declined rapidly....
Four nitro- and fluorobenzamides (1–4) have been synthesized in good yields from fluoro-substituted benzoyl chloride with 4-amino-1-benzylpiperidine. In vitro studies showed that these compounds high affinities to σ receptors. N-(N-Benzylpiperidin-4-yl)-2-fluorobenzamide (3), particular, bound receptors affinity (Ki = 3.4 nM, guinea pig brain membranes) selectivity (σ-2σ-1 120). It was, therefore, labeled 18F evaluated as a receptor radioligand....
We report on the preparation of a hypoxia marker 2-(2-nitroimidazol-1[H]-yl)-N-(3-fluoropropyl)acetamide (EF1) and its 18F analog, 2-(2-nitroimidazol-1[H]-yl)-N-(3-[18F]fluoropropyl)acetamide ([18F]-EF1). Two methods for 3-fluoropropylamine, EF1 side chain, are described. [18F]-EF1 was prepared with radiochemical yield 2% by nucleophilic substitution bromine in 2-(2-nitroimidazol-1[H]-yl)-N-(3-bromopropyl)acetamide (EBr1) carrier-added DMSO at 120°C. Our results demonstrate clinically...
In vitro studies showed that MK-912 ((2S, 12bS)1',3'-dimethylspiro(1,3,4,5',6,6',7,12b-octahydro -2H-benzo[b]furo[2,3-a]quinolizine)-2,4'-pyrimidin-2'-one) is a potent alpha2-adrenergic receptor antagonist with high affinity (Ki = 0.42, 0.26 and 0.03 nM to alpha2A, alpha2B alpha2C, respectively) selectivity (alpha2A/alpha1A 240; alpha2A/D-1 3600; alpha2A/D-2 3500; alpha2A/5-HT1 700; alpha2A/5-HT2 4100). The compound was labeled 11C evaluated in rodents monkey as specific radioligand for...
Epigenetic dysfunction is implicated in many neurologic, psychiatric and oncologic diseases. Consequently, histone deacetylases (HDACs) inhibitors have been developed as therapeutic imaging agents for these However, only a few radiotracers HDACs the central nervous system (CNS). We report herein synthesis evaluation of [18F]INER-1577-3 ([18F]5) an agent CNS.[18F]INER-1577-3 was synthesized by two methods: one-step (A) two-step (B) methods. Briefly, radiofluorination corresponding precursors...
High performance liquid chromatography coupled with tandem mass spectrometry was developed and validated as a method for the analysis of fluorinated histone deacetylase inhibitors (F-HDACi), then employed to study their metabolism in biosystems. Four HDACi analogs labeled positron emission nuclide 18F constitute group potential tomography imaging agents, which were by Institute Nuclear Energy Research (INER) coded INER-1577 #1, #2, #3, #4 during animal studies diagnosis dementia. The found...
Abstract Methyl‐N‐carbobenzoxy‐β‐ 131 I‐D‐alaninate ( 2 ) was synthesized by the melt method. Partial hydrolysis of compound gave methyl β‐ 3 ). Hydrolysis with N HCl I‐D‐alanine. The 123 I and 125 labelled compounds were same