PNU-282987

PNU-282987 is a potent and selective agonist of the α7 subtype of neural nicotinic acetylcholine receptors (α7 nAChR). It exhibits high affinity for α7 nAChRs (Ki ≈ 26 nM) and shows minimal activity at other receptor types except for weak antagonism at 5‑HT3 receptors. In preclinical studies, PNU‑282987 enhances GABAergic synaptic activity in the hippocampus, improves sensory gating deficits, and demonstrates nootropic effects such as improved performance in cognitive tasks. It has been investigated as a potential therapy for schizophrenia due to its ability to modulate hippocampal neurotransmission and restore auditory gating deficits in animal models. Additional research suggests neuroprotective effects in models of Parkinson’s disease, stroke, glaucoma-induced retinal damage, acute lung injury, and diabetic wound healing through anti-inflammatory mechanisms or neurogenesis induction. However, it is not suitable for human use due to excessive inhibition of the hERG potassium channel (a cardiac antitarget), which poses safety concerns[1][2][3][4][5][6][7][8].

Other names

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamide hydrochloride