Now showing items 1-6 of 6

    • 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 ...
    • 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 ...
    • 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. ...
    • Imaging Evaluation of 5HT\(_{2C}\) Agonists, [\(^{11}\)C]WAY-163909 and [\(^{11}\)C]Vabicaserin, Formed by Pictet–Spengler Cyclization 

      Neelamegam, Ramesh; Hellenbrand, Tim; Schroeder, Frederick A; Wang, Changning; Hooker, Jacob M (American Chemical Society (ACS), 2014)
      The serotonin subtype 2C (5HT\(_{2C}\)) receptor is an emerging and promising drug target to treat several disorders of the human central nervous system. In this current report, two potent and selective 5HT\(_{2C}\) full ...
    • Radiosynthesis and Evaluation of [11C]EMPA as a Potential PET Tracer for Orexin 2 Receptors 

      Wang, Changning; Moseley, Christian K.; Carlin, Stephen M.; Wilson, Colin M.; Neelamegam, Ramesh; Hooker, Jacob M (Elsevier BV, 2013)
      EMPA is a selective antagonist of orexin 2 (OX2) receptors. Previous literature with [3H]-EMPA suggest that it may be used as an imaging agent for OX2 receptors; however, brain penetration is known to be modest. To evaluate ...
    • Synthesis and Evaluation of Methylated Arylazepine Compounds for PET Imaging of 5-HT 2c Receptors 

      Granda, Michael L.; Carlin, Stephen M.; Moseley, Christian K.; Neelamegam, Ramesh; Mandeville, Joseph B.; Hooker, Jacob M (American Chemical Society (ACS), 2013)
      The serotonin 5-HT2c receptor is implicated in a number of diseases including obesity, depression, anxiety, and schizophrenia. In order to ascribe the role of 5-HT2c in these diseases, a method for measuring 5-HT2c density ...