PNU-282987 is an α7 nAChR agonist with an EC50 of 154 nM against the a7-5HT3 chimera. Up to concentrations of 100 uM, PNU-282987 displayed no agonist activity and negligible antagonistic activity (60 uM) toward the neuromuscular junction form of the receptor and the ganglionic nAChR (a3b4). PNU-282987 is a functional antagonist of the 5-HT3 receptor at an IC50 of 4.5 uM. (1)

Cotreatment of PC12 cells with nAChR modulator PNU120596 and PNU-282987 significantly induces ERK1/2 phosphorylation. (2) In a chloral hydrate-anesthetized rat model, PNU-282987 was shown to restore amphetamine-induced sensory gating deficit and may have implications in the treatment of schizophrenia. (3)