BUY PNU 282987

PNU 282987. Selective Agonist of alpha7nAChR

Nicotinic acetylcholine receptors (nAChRs) are members of the Cys-Loop ligand-gated ion channel superfamily, located both in the peripheral and central nervous systems (PNS and CNS, respectively). These receptors, existing as both homopentameric and heteropentameric transmembrane ion channels, are validated therapeutic targets for various CNS pathologies.
PNU 282987 is a selective agonist of alpha7 nAChRs, which are predominantly found in the central nervous system. It enhances alpha7 nAChRs currents with an EC₅₀ of 5.6 μM in Xenopus oocytes and has a Ki of 26 nM in rat alpha7 nAChR.
Selective alpha7 nAChR agonists, such as PNU-282987, improve performance in sensory gating, novel object recognition, social recognition, water maze performance, or inhibitory avoidance models of cognitive function. Given these roles, targeting alpha7 nAChRs has been considered as a viable strategy for a variety of diseases involving cognitive deficits and neurodegeneration.

Ion Channel Modulators; Nicotinic Acetylcholine Receptor Activators.