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PNU 120596 is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor (nAChR), increasing agonist-evoked calcium flux (EC50 = 216 nM).1 It has no detectable effect on α4β2, α3β4, or α9β10 nAChRs. PNU-120596 increases the frequency of ACh-evoked GABAergic postsynaptic currents in rat hippocampal slices and improves the auditory gating deficit caused by amphetamine in rats.1,2 It also reduces the cortical/subcortical infarct volume caused by transient focal cerebral ischemia in rats.3
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1. A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: In vitro and in vivo characterization. J. Neurosci. 25(17), 4396-4405 (2015).
2. An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-
3. A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischaemia. Br. J. Pharmacol. 169(8), 1862-1878 (2013).