PNU-120596

PNU-120596 is a potent and selective positive allosteric α7 neuronal nicotinic acetylcholine receptors modulator with an EC50 of 0.2 μM. PNU-120596 has no detectable effect on α4β2, α3β4 and α9α10 receptors. Discovered in a high-throughput screen, PNU-120596 enhanced agonist-evoked calcium flux mediated by an engineered variant of the human α7 nAChR. Electrophysiology studies demonstrated that PNU-120596 increased peak agonist-evoked currents mediated by wild-type receptors and also proved a pronounced prolongation of the triggered response in the continued presence of agonist.