Technology ID
              TAB-3761
          Truncated (N)-Methanocarba Nucleosides as Al Adenosine Receptor Agonists and Partial Agonists: Receptor Docking and Potent Anticonvulsant Activity for the Treatment of Various Conditions
E-Numbers
          E-166-2012-0
              Lead Inventor
          Jacobson, Kenneth
              Lead IC
          NIDDK
              Co-Inventors
          Tosh, Dilip
              ICs
          NIDDK
              Applications
          Therapeutics
              Therapeutic Areas
          Psychiatry/Mental Health
          Ophthalmology
          Oncology
          Neurology
          Infectious Disease
          Endocrinology
          Dental
          Cardiology
              This technology includes A1AR-selective agonists which are full or partial agonists of the A1AR and are being considered for treatment of various conditions: seizures, stroke, diabetes, pain, cardio-protection and arrhythmias. A1AR agonists are highly neuroprotective in ischemic and epileptic models. A1AR agonists are also being explored for antidepressant, antianxiety, and other neuropsychiatric effects, due to their presynaptic action to decrease the release of excitatory amino acids in the brain. However, peripheral cardiovascular side effects have prevented the introduction of A1AR agonist for treating disorders of the central nervous system (CNS).
      
  Commercial Applications
              For use in clinical diagnostics or therapeutically for the treatment of various conditions, such as stroke, epilepsy and pain.
      Competitive Advantages
              This class of compounds produced some full agonists of the human A1AR of moderate affinity and selectivity (>10-fold vs. A2AAR and A3AR).
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