PNU 282987

Selective Agonist of α7 nAChR
    Cat #: P-110
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 264.75
    Purity: >98%
    Effective concentration EC50 ~ 5 μM.
    • PNU 282987
    Chemical name N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide.
    Molecular formula C14H17ClN2O.
    CAS No.: 123464-89-1.
    Activity PNU 282987 is a selective agonist of α7 nicotinic acetylcholine receptor (nAChR)1-2, with an EC50 of 5.6 μM in Xenopus oocytes3 and Ki of 26 nM in rat α7 nAChR1. Via modulating/enhancing hippocampal GABAergic neurotransmission, PNU 282987 improves auditory gating and enhances hippocampal oscillatory activity and therefore may offer a potential pharmacotherapy in the treatment of schizophrenia1.
    1. Hajós, M. et al. (2005) J. Pharmacol. Exp. Ther. 312, 1213.
    2. Bodnar, A.L. et al. (2005) J. Med.Chem. 48, 905.
    3. Grønlien, J.H. et al. (2007) Mol. Pharmacol. 72, 715.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
    Our bioassay
    • PNU 282987
      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.
    References - Scientific background
    1. Kombo, D.C. et al. (2011) Eur. J. Med. Chem. In Press.
    2. Hajós, M. et al. (2005) J. Pharmacol. Exp. Ther. 312, 1213.
    3. Bodnar, A.L. et al. (2005) J. Med.Chem. 48, 905.
    4. Grønlien, J.H. et al. (2007) Mol. Pharmacol. 72, 715.
    5. Levin, E.D. et al (2002) Curr. Drug Targets CNS Neurol. Disord. 1, 423.
    6. Gotti, C. et al (2006) Curr. Pharm. Des. 12, 407.
    Scientific background

    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.

    Target α7 nAChR
    Last update: 04/06/2020

    PNU 282987 (#P-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background


    in vivo
    1. Mouse intraperitoneal injections.
      Gupta, D. et al. (2018) J. Biol. Chem. 293, 20295.
    1. Rat INS-1 insulinoma cells.
      Gupta, D. et al. (2018) J. Biol. Chem. 293, 20295.
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