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Evaluation of Potential PET Imaging Probes for the Orexin 2 Receptors
(Elsevier BV, 2013)
A wide range of central nervous system (CNS) disorders, particularly those related to sleep, are associated with the abnormal function of orexin (OX) receptors. Several orexin receptor antagonists have been reported in ...
Class I HDAC imaging using [3H]CI-994 autoradiography
(Landes Bioscience, 2013)
[3H]CI-994, a radioactive isotopologue of the benzamide CI-994, a class I histone deacetylase inhibitor (HDACi), was evaluated as an autoradiography probe for ex vivo labeling and localizing of class I HDAC (isoforms 1–3) ...
Application of Palladium-Mediated 18F-Fluorination to PET Radiotracer Development: Overcoming Hurdles to Translation
(Public Library of Science, 2013)
New chemistry methods for the synthesis of radiolabeled small molecules have the potential to impact clinical positron emission tomography (PET) imaging, if they can be successfully translated. However, progression of ...
Radionuclide Labeling and Evaluation of Candidate Radioligands for PET Imaging of Histone Deacetylase in the Brain
(Elsevier BV, 2013)
Histone deacetylases (HDACs) regulate gene expression by inducing conformational changes in chromatin. Ever since the discovery of a naturally occurring HDAC inhibitor, trichostatin A (TSA) stimulated the recent development ...
Whole-Body Pharmacokinetics of HDAC Inhibitor Drugs, Butyric Acid, Valproic Acid and 4-Phenylbutyric Acid Measured with Carbon-11 Labeled Analogs by PET
(Elsevier BV, 2013)
The fatty acids, n-butyric acid (BA), 4-phenylbutyric acid (PBA) and valproic acid (VPA, 2-propylpentanoic acid) have been used for many years in the treatment of a variety of CNS and peripheral organ diseases including ...
FDG-PET Imaging Reveals Local Brain Glucose Utilization Is Altered by Class I Histone Deacetylase Inhibitors
(Elsevier BV, 2013)
The purpose of this work – the first of its kind – was to evaluate the impact of chronic selective histone deacetylase (HDAC) inhibitor treatment on brain activity using uptake of the radioligand 18F-fluorodeoxyglucose and ...
Identification of Pseudomonas aeruginosa Phenazines that Kill Caenorhabditis elegans
(Public Library of Science, 2013)
Pathogenic microbes employ a variety of methods to overcome host defenses, including the production and dispersal of molecules that are toxic to their hosts. Pseudomonas aeruginosa, a Gram-negative bacterium, is a pathogen ...