Every lot is tried & tested in a relevant biological assay.
- Alomone Labs PNU 282987 activates α7 nicotinic AChR heterologously expressed in Xenopus oocytes and at high concentration inhibits the activation by acetylcholine.A. Current traces of α7 nicotinic AChR channels activity at -60 mV holding potential. Currents were elicited by application of 100 µM acetylcholine every 50 seconds. Inhibition of these induced currents was achieved upon perfusion of 40 µM PNU 282987 (#P-110), as indicated by the horizontal bar. B. Superimposed traces of α7 nicotinic ACh channel current in the absence or presence of 0.5 μM, 1 μM or 10 μM PNU 282987, as indicated.
- Kombo, D.C. et al. (2011) Eur. J. Med. Chem. In Press.
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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 pathologies1.
PNU 282987 is a selective agonist of α7 nAChRs2-3, which are predominantly found in the central nervous system. It enhances α7 nAChRs currents with an EC50 of 5.6 µM in Xenopus oocytes4 and has a Ki of 26 nM in rat α7 nAChR2. Selective α7 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 function4. Given these roles, targeting α7 nAChRs has been considered as a viable strategy for a variety of diseases involving cognitive deficits and neurodegeneration5-6.
PNU 282987 (#P-110) is a highly pure, synthetic, and biologically active compound.