AQW-051 is a novel, potent and selective, orally bioavailable, brain-penetrant α7 nAChR partial agonist with pKd of 7.56; displays high selectivity (>100-fold) over other nACh receptors; stimulates calcium influx in GH3–ha7-22 cells recombinantly expressing the human α7-nACh receptor with pEC50 of 7.41; facilitates learning/memory performance in mice; reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys.
