Jacobson, Kenneth (NIDDK)
Lechleiter, James (University of Texas Health Science Center)
Liston, Theodore (Astrocyte Pharmaceuticals, Inc)
This technology includes MRS4322, which is an A3 agonist that is currently being evaluated for treatment of traumatic brain injury. Although its affinity in the receptor is in the micromolar range, it enters the brain in sufficient concentration to activate a protective CNS receptor, A3 adenosine receptor. Potential applications of such A3 agonists could also include neurodegenerative conditions.
This compound produced fully agonizes the human A3 adenosine receptor with µmolar affinity with moderate selectivity vs. other adenosine receptors and displays the appropriate physicochemical properties for effective agonism and bioavailability in vivo.