Jacobson, Kenneth (NIDDK)
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).
For use in clinical diagnostics or therapeutically for the treatment of various conditions, such as stroke, epilepsy and pain.
This class of compounds produced some full agonists of the human A1AR of moderate affinity and selectivity (>10-fold vs. A2AAR and A3AR).