Browsing HMS Scholarly Articles by FAS Department "Chemistry and Chemical Biology"
Now showing items 1-20 of 24
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[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 ... -
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 ... -
Characterisation of [11C]PR04.MZ in Papio Anubis Baboon: A Selective High-Affinity Radioligand for Quantitative Imaging of the Dopamine Transporter
(Elsevier BV, 2012)N-(4-fluorobut-2-yn-1-yl)-2β-carbomethoxy-3β-(4′-tolyl)nortropane (PR04.MZ, 1) is a PET radioligand for the non-invasive exploration of the function of the cerebral dopamine transporter (DAT). A reliable automated process ... -
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) ... -
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 ... -
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 ... -
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 ... -
Histone Deacetylase Inhibitor MS-275 Exhibits Poor Brain Penetration: Pharmacokinetic Studies of [ 11 C]MS-275 using Positron Emission Tomography
(American Chemical Society (ACS), 2010)MS-275 (entinostat) is a histone deacetylase (HDAC) inhibitor currently in clinical trials for the treatment of several types of cancer. Recent reports have noted that MS-275 can cross the blood−brain barrier (BBB) 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 ... -
In Vivo Photoactivation Without “Light”: Use of Cherenkov Radiation to Overcome the Penetration Limit of Light
(Springer Nature, 2011)Purpose: The poor tissue penetration of visible light has been a major barrier for optical imaging, photoactivatable conversions, and photodynamic therapy for in vivo targets with depths beyond 10 mm. In this report, as a ... -
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 ... -
Nanowire-Mediated Delivery Enables Functional Interrogation of Primary Immune Cells: Application to the Analysis of Chronic Lymphocytic Leukemia
(American ChemicalSociety, 2012)A circuit level understanding of immune cells and hematological cancers has been severely impeded by a lack of techniques that enable intracellular perturbation without significantly altering cell viability and function. ... -
Non-Proteinogenic Amino Acids in Lacticin 481 Analogues Result in More Potent Inhibition of Peptidoglycan Transglycosylation
(American Chemical Society, 2012)Lantibiotics are ribosomally synthesized and post-translationally modified peptide natural products that contain the thioether structures lanthionine and methyllanthionine and exert potent antimicrobial activity against ... -
One-Pot, Direct Incorporation of [11 C]CO 2 into Carbamates
(Wiley-Blackwell, 2009)Why beat about the bush? An operationally simple and mild reaction based on the direct fixation of 11CO2 with 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) has been developed for the synthesis of 11C-labeled carbamates at 75 °C ... -
Pharmacokinetics of the Potent Hallucinogen, Salvinorin A in Primates Parallels the Rapid Onset and Short Duration of Effects in Humans
(Elsevier BV, 2008)Salvia divinorum, a mint plant originally used by the Mazatecs of Oaxaca, Mexico in spiritual rituals has gained popularity, in smoked form, as a legal hallucinogen in the United States and Europe. Abuse results in rapid ... -
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 ... -
Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons
(American Chemical Society (ACS), 2010)The front-line tuberculosis (TB) chemotherapeutics isoniazid (INH), rifampicin (RIF), and pyrazinamide (PZA) have been labeled with carbon-11 and the biodistribution of each labeled drug has been determined in baboons using ... -
Radiosynthesis of C-11 Labeled Auxin (3-Indolyl[1-11C]acetic Acid) and Its Derivatives from Gramine
(Wiley-Blackwell, 2011)3-Indolylacetic acid (IAA) is the major auxin in higher plants and plays a key role in plant growth and development. We report the rapid radiolabeling of the important plant hormone using carbon-11 (half life: 20.4 min) ... -
Rapid Chemoselective Bioconjugation Through Oxidative Coupling of Anilines and Aminophenols
(American Chemical Society (ACS), 2011)A highly efficient protein bioconjugation method is described involving addition of anilines to o-aminophenols in the presence of sodium periodate. The reaction takes place in aqueous buffer at pH 6.5 and can reach high ... -
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 ...