Browsing by Author "Hooker, Jacob"

Now showing items 1-20 of 54

    • [11C]PR04.MZ, a Promising DAT Ligand for Low Concentration Imaging: Synthesis, Efficient 11C-O-Methylation and Initial Small Animal PET Studies 

      Riss, Patrick J.; Hooker, Jacob M; Alexoff, David; Kim, Sung-Won; Fowler, Joanna S.; Rösch, Frank (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 ...

    • 11CO2 Fixation: A Renaissance in PET Radiochemistry 

      Rotstein, Benjamin H; Liang, Steven; Holland, Jason P; Collier, Thomas L; Hooker, Jacob M; Wilson, Alan A.; Vasdev, Neil (Royal Society of Chemistry, 2013)
      Carbon-11 labelled carbon dioxide is the cyclotron-generated feedstock reagent for most positron emission tomography (PET) tracers using this radionuclide. Most carbon-11 labels, however, are installed using derivative ...

    • Application of Palladium-Mediated 18F-Fluorination to PET Radiotracer Development: Overcoming Hurdles to Translation 

      Kamlet, Adam; Neumann, Constanze Nicole; Lee, Eunsung; Carlin, Stephen M.; Moseley, Christian K.; Stephenson, Nickeisha A; Hooker, Jacob M; Ritter, Tobias (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 ...

    • Brain-Penetrant LSD1 Inhibitors Can Block Memory Consolidation 

      Neelamegam, Ramesh; Ricq, Emily Louise; Malvaez, Melissa; Patnaik, Debasis; Norton, Stephanie; Carlin, Stephen M.; Hill, Ian Thomas; Wood, Marcelo A.; Haggarty, Stephen John; Hooker, Jacob M (American Chemical Society (ACS), 2012)
      Modulation of histone modifications in the brain may represent a new mechanism for brain disorder therapy. Post-translational modifications of histones regulate gene expression, affecting major cellular processes such as ...

    • Characterisation of [11C]PR04.MZ in Papio Anubis Baboon: A Selective High-Affinity Radioligand for Quantitative Imaging of the Dopamine Transporter 

      Riss, Patrick J.; Hooker, Jacob M; Shea, Colleen; Xu, Youwen; Carter, Pauline; Warner, Donald; Ferrari, Valentina; Kim, Sung-Won; Aigbirhio, Franklin I.; Fowler, Joanna S.; Roesch, Frank (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 ...

    • Chemical Neurobiology of the Histone Lysine Demethylase KDM1A 

      Ricq, Emily (2016-05-18)
      Epigenetic mechanisms regulate gene expression and mediate interactions between genetic factors and environmental exposures. The enzymes responsible for epigenetic regulation may thus be important therapeutic targets for ...

    • Class I HDAC imaging using [3H]CI-994 autoradiography 

      Wang, Yajie; Zhang, Yan-Ling; Hennig, Krista; Gale, Jennifer P.; Hong, Yijia; Cha, Anna; Riley, Misha; Wagner, Florence; Haggarty, Stephen John; Holson, Edward; Hooker, Jacob M (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) ...

    • Combination Therapy: Histone Deacetylase Inhibitors and Platinum-Based Chemotherapeutics for Cancer 

      Diyabalanage, Himashinie V K; Granda, Michael L.; Hooker, Jacob M (Elsevier BV, 2013)
      One of the most promising strategies to increase the efficacy of standard chemotherapy drugs is by combining them with low doses of histone deacetylases inhibitors (HDACis). Regarded as chemosensitizers, the addition of ...

    • Concerted nucleophilic aromatic substitution with 19F− and 18F− 

      Neumann, Constanze N.; Hooker, Jacob M.; Ritter, Tobias (2016)
      Nucleophilic aromatic substitution (SNAr) is widely used by organic chemists to functionalize aromatic molecules, and it is the most commonly used method to generate arenes that contain a 18F for use in PET imaging.1 A ...

    • Cue-Induced Dopamine Release Predicts Cocaine Preference: Positron Emission Tomography Studies in Freely Moving Rodents 

      Schiffer, W. K.; Liebling, C. N. B.; Reiszel, C.; Hooker, Jacob M; Brodie, J. D.; Dewey, S. L. (Society for Neuroscience, 2009)
      Positron emission tomography studies in drug-addicted patients have shown that exposure to drug-related cues increases striatal dopamine, which displaces binding of the D2 ligand, [11C]-raclopride. However, it is not known ...

    • Design, Synthesis, and Evaluation of Hydroxamic Acid-Based Molecular Probes for In Vivo Imaging of Histone Deacetylase (HDAC) in Brain 

      Hooker, Jacob M; Wang, Changning; Eessalu, Thomas E.; Barth, Vanessa N.; Mitch, Charles H.; Wagner, Florence F.; Hong, Yijia; Neelamegam, Ramesh; Schroeder, Frederick A; Holson, Edward B.; Haggarty, Stephen John (e-Century Publishing, 2014)
      Hydroxamic acid-based histone deacetylase inhibitors (HDACis) are a class of molecules with therapeutic potential currently reflected in the use of suberoylanilide hydroxamic acid (SAHA; Vorinostat) to treat cutaneous ...

    • Dopamine D1 signaling organizes network dynamics underlying working memory 

      Roffman, Joshua L.; Tanner, Alexandra S.; Eryilmaz, Hamdi; Rodriguez-Thompson, Anais; Silverstein, Noah J.; Ho, New Fei; Nitenson, Adam Z.; Chonde, Daniel B.; Greve, Douglas N.; Abi-Dargham, Anissa; Buckner, Randy L.; Manoach, Dara S.; Rosen, Bruce R.; Hooker, Jacob M.; Catana, Ciprian (American Association for the Advancement of Science, 2016)
      Local prefrontal dopamine signaling supports working memory by tuning pyramidal neurons to task-relevant stimuli. Enabled by simultaneous positron emission tomography–magnetic resonance imaging (PET-MRI), we determined ...

    • Effects of ferumoxytol on quantitative PET measurements in simultaneous PET/MR whole-body imaging: a pilot study in a baboon model 

      Borra, Ronald JH; Cho, Hoon-Sung; Bowen, Spencer L; Attenberger, Ulrike; Arabasz, Grae; Catana, Ciprian; Josephson, Lee; Rosen, Bruce R; Guimaraes, Alexander R; Hooker, Jacob M (Springer International Publishing, 2015)
      Background: Simultaneous PET/MR imaging depends on MR-derived attenuation maps (mu-maps) for accurate attenuation correction of PET data. Currently, these maps are derived from gradient-echo-based MR sequences, which are ...

    • Effects of Modafinil on Dopamine and Dopamine Transporters in the Male Human Brain 

      Volkow, Nora D.; Fowler, Joanna S.; Logan, Jean; Alexoff, David; Zhu, Wei; Telang, Frank; Wang, Gene-Jack; Jayne, Millard; Hooker, Jacob M; Wong, Christopher; Hubbard, Barbara; Carter, Pauline; Warner, Donald; King, Payton; Shea, Colleen; Xu, Youwen; Muench, Lisa; Apelskog-Torres, Karen (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 ...

    • An Efficient and Practical Radiosynthesis of [11C] Temozolomide 

      Moseley, Christian K.; Carlin, Stephen M.; Neelamegam, Ramesh; Hooker, Jacob M (American Chemical Society (ACS), 2012)
      Temozolomide (TMZ) is a prodrug for an alkylating agent used for the treatment of malignant brain tumors. A positron emitting version, [11C]TMZ, has been utilized to help elucidate the mechanism and biodistribution of TMZ. ...

    • Evaluation of [11C]metergoline as a PET Radiotracer for 5HTR in Nonhuman Primates 

      Hooker, Jacob M; Kim, Sung Won; Reibel, Achim T.; Alexoff, David; Xu, Youwen; Shea, Colleen (Elsevier BV, 2010)
      Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [11C]Metergoline had moderate ...

    • Evaluation of Potential PET Imaging Probes for the Orexin 2 Receptors 

      Wang, Changning; Wilson, Colin M.; Moseley, Christian K.; Carlin, Stephen M.; Hsu, Shirley; Arabasz, Grae; Schroeder, Frederick A; Sander, Christin Y.; Hooker, Jacob M (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 

      Schroeder, Frederick A; Chonde, Daniel Burje; Riley, Misha M.; Moseley, Christian K.; Granda, Michael L.; Wilson, Colin M.; Wagner, Florence F.; Zhang, Yan-Ling; Gale, Jennifer; Holson, Edward B.; Haggarty, Stephen John; Hooker, Jacob M (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 ...

    • A Fluoride-Derived Electrophilic Late-Stage Fluorination Reagent for PET Imaging 

      Lee, Eunsung; Kamlet, Adam Seth; Powers, David C.; Neumann, Constanze Nicole; Boursalian, Gregory Bagrad; Furuya, Takeru; Choi, Daniel C.; Hooker, Jacob M.; Ritter, Tobias (American Association for the Advancement of Science, 2011)
      The unnatural isotope fluorine-18 \((^{18}F)\) is used as a positron emitter in molecular imaging. Currently, many potentially useful \(^{18}F\)-labeled probe molecules are inaccessible for imaging because no fluorination ...

    • Glial activation colocalizes with structural abnormalities in amyotrophic lateral sclerosis 

      Alshikho, Mohamad J.; Zürcher, Nicole R.; Loggia, Marco L.; Cernasov, Paul; Chonde, Daniel B.; Izquierdo Garcia, David; Yasek, Julia E.; Akeju, Oluwaseun; Catana, Ciprian; Rosen, Bruce R.; Cudkowicz, Merit E.; Hooker, Jacob M.; Atassi, Nazem (Lippincott Williams & Wilkins, 2016)
      Objective: In this cross-sectional study, we aimed to evaluate brain structural abnormalities in relation to glial activation in the same cohort of participants. Methods: Ten individuals with amyotrophic lateral sclerosis ...