A5025961784- Radiopharmaceutical Chemistry and Applications
- Prostate Cancer Treatment and Research
- Medical Imaging Techniques and Applications
- Neurotransmitter Receptor Influence on Behavior
- Peptidase Inhibition and Analysis
- Neuroscience and Neuropharmacology Research
- Parkinson's Disease Mechanisms and Treatments
- Receptor Mechanisms and Signaling
- Chemical Reactions and Isotopes
- Amino Acid Enzymes and Metabolism
- Medical Imaging and Pathology Studies
- Neuropeptides and Animal Physiology
- Neurological disorders and treatments
- Metabolism and Genetic Disorders
- Forensic Toxicology and Drug Analysis
- Pharmacological Receptor Mechanisms and Effects
- Bone health and treatments
- Functional Brain Connectivity Studies
- Ion channel regulation and function
- Anesthesia and Neurotoxicity Research
- Lanthanide and Transition Metal Complexes
- Alzheimer's disease research and treatments
- Nicotinic Acetylcholine Receptors Study
- Cancer Treatment and Pharmacology
- Coffee research and impacts
Brookhaven National Laboratory
1994-2015
National Institute on Drug Abuse
2004-2009
Stony Brook University
2003
Brookhaven College
1993
New York University
1993
Modafinil, a wake-promoting drug used to treat narcolepsy, is increasingly being as cognitive enhancer. Although initially launched distinct from stimulants that increase extracellular dopamine by targeting transporters, recent preclinical studies suggest otherwise.To measure the acute effects of modafinil at doses therapeutically (200 mg and 400 given orally) on transporters in male human brain.Positron emission tomography with [(11)C]raclopride (D(2)/D(3) radioligand sensitive changes...
Background Methamphetamine is one of the most toxic drugs abuse, which may reflect its distribution and accumulation in body. However no studies have measured methamphetamine's organ human Methods Positron Emission Tomography (PET) was used conjunction with [11C]d-methamphetamine to measure whole-body bioavailability as assessed by peak uptake (% Dose/cc), rate clearance (time reach 50% peak-clearance) (area under curve) healthy participants (9 Caucasians 10 African Americans). Results...
Caffeine, the most widely consumed psychoactive substance in world, is used to promote wakefulness and enhance alertness. Like other wake-promoting drugs (stimulants modafinil), caffeine enhances dopamine (DA) signaling brain, which it does predominantly by antagonizing adenosine A2A receptors (A2AR). However, unclear if caffeine, at doses humans, increases DA release or whether modulates functions of postsynaptic through its interaction with receptors, modulate them. We positron emission...
SynapseVolume 53, Issue 3 p. 184-189 6-[18F]Fluoro-A-85380, a new PET tracer for the nicotinic acetylcholine receptor: Studies in human brain and vivo demonstration of specific binding white matter Yu-Shin Ding, Corresponding Author Ding Chemistry Department, Brookhaven National Laboratory, Upton, New YorkChemistry NY 11973Search more papers by this authorJoanna S. Fowler, Joanna Fowler YorkSearch authorJean Logan, Jean Logan authorGene-Jack Wang, Gene-Jack Wang Medical authorFrank Telang,...
Abstract Reboxetine is a specific norepinephrine transporter (NET) inhibitor and has been marketed in several countries as racemic mixture of the (R,R) (S,S) enantiomers for treatment depression. Its methyl analog (methylreboxetine, MRB) shown to be more potent than reboxetine itself. We developed nine‐step synthetic procedure prepare normethyl precursor, which was used synthesize [ 11 C]O‐methylreboxetine ([ C]MRB). also convenient resolution method using chiral HPLC column resolve...
One of the major mechanisms for terminating actions catecholamines and vasoactive dietary amines is oxidation by monoamine oxidase (MAO). Smokers have been shown to reduced levels brain MAO, leading speculation that MAO inhibition tobacco smoke may underlie some behavioral epidemiological features smoking. Because smoking exposes peripheral organs as well MAO-inhibitory compounds, we questioned whether smokers would also in organs. Here compared B nonsmokers using positron emission...
The possibility of slowing the progression Parkinson's disease (PD) with inhibitors monoamine oxidase B (MAO B) has stimulated development new MAO inhibitor drugs. Ro 19 6327 is a highly selective currently under clinical investigation. We used positron emission tomography (PET) and tracer [11C]L-deprenyl to determine degree reversibility human brain inhibition by in six early patients who were treated different doses (25 mg [n = 3], 50 2], 100 1]; 0.34 1.4 mg/kg) every 12 hours for 1 week....
Bone metastasis in cancer patients is a major disease advancement for various types of cancer. Previously, [68Ga]Ga-HBED-CC-bisphosphonate ([68Ga]Ga-P15-041) showed excellent bone uptake and efficient detection patients. To accommodate different α- or β–-emitting metals radionuclide therapy, novel DOTA-HBED-CC-bisphosphonate (P15-073, 1) was prepared the corresponding [68Ga]Ga-1 [177Lu]Lu-1 were successfully synthesized high yields purity. Gallium-68 conjugation to HBED-CC at room...
Although important aspects of whole-plant carbon allocation in crop plants (e.g., to grain) occur late development when the are large, techniques study transport and processes have not been adapted for large plants. Positron emission tomography (PET), developed dynamic imaging medicine, has applied plant studies measure patterns carbohydrates, nutrients, phytohormones labeled with positron-emitting radioisotopes. However, cost PET its limitation smaller restricted use biology. Here we...
Dopamine D3 receptor (D3R) antagonists may be effective medications for multiple substance use disorders (SUDs). However, no selective D3R are currently available clinical testing. Buspirone, originally characterized as a 5-HT1A partial agonist and used an anxiolytic, also binds to D4R with high affinity, lower affinity D2R, interferes cocaine reward. Here we PET [11C]PHNO (D3R-preferring radioligand), [11C]raclopride (D2R/D3R radioligand) [11C]NNC-112 (D1R measure occupancy of oral...
Positron emission tomography (PET) imaging using 68Ga-labeled bisphosphonates to target bone metastasis could be a valuable tool in cancer diagnosis and monitoring therapeutic treatment. A 68Ga labeled ligand, N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid (HBED-CC) containing one bisphosphonate group (HBED-CC-BP, 1) was prepared evaluated. The new 1, reacted rapidly form [68Ga]Ga-1, via complexing with [68Ga]GaCl3 eluted from commercially available 68Ge/68Ga...
Prostate-specific membrane antigen (PSMA) is a promising target for the diagnosis and radionuclide therapy of prostate cancer. This study reports conversion previously reported 68Ga-imaging agent, [68Ga]Ga-P16-093, to Lu-177 therapeutic agent. Substitution HBED-CC metal chelating group with DOTA(GA)2 led P17-087 (4) P17-088 (7). Both agents showed excellent PSMA binding affinity (IC50 = 10–30 nM) comparable that recently FDA-approved [177Lu]Lu-PSMA-617 (Pluvicto). Biodistribution studies in...