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Metabolic Changes in the Rodent Brain after Acute Administration of Salvinorin A
(Springer Nature, 2009)
Purpose: Salvinorin A (SA) is a potent and highly selective kappa-opioid receptor (KOR) agonist with rapid kinetics and commensurate behavioral effects; however, brain regions associated with these effects have not been ...
[11C]PR04.MZ, a Promising DAT Ligand for Low Concentration Imaging: Synthesis, Efficient 11C-O-Methylation and Initial Small Animal PET Studies
(Elsevier BV, 2009)
PR04.MZ was designed as a highly selective dopamine transporter inhibitor, derived from natural cocaine. Its binding profile indicates that [11C]PR04.MZ may be suited as a PET radioligand for the non-invasive exploration ...
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 ...
Effects of Modafinil on Dopamine and Dopamine Transporters in the Male Human Brain
(American Medical Association (AMA), 2009)
Context: Modafinil, a wake-promoting drug used to treat narcolepsy, is increasingly being used as a cognitive enhancer. Although initially launched as distinct from stimulants that increase extracellular dopamine by targeting ...
Reinvestigation of the Synthesis and Evaluation of [N-methyl-11C]vorozole, a Radiotracer Targeting Cytochrome P450 Aromatase
(Elsevier BV, 2009)
Introduction: We reinvestigated the synthesis of [N-methyl-11C]vorozole, a radiotracer for aromatase, and discovered the presence of an N-methyl isomer which was not removed in the original purification method. Herein we ...
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 ...
Visualizing Epigenetics: Current Advances and Advantages in HDAC PET Imaging Techniques
(Elsevier BV, 2014)
Abnormal gene regulation as a consequence of flawed epigenetic mechanisms may be central to the initiation and persistence of many human diseases. However, the association of epigenetic dysfunction with disease and the ...
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 ...