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RJR 2403 oxalate

Rivanicline oxalate

An Agonist of α4/β2 nAChRs

Cat #: R-115
Alternative Name Rivanicline oxalate
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 252.3
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Chemical name (E)-N-Methyl-4-(3-pyridinyl)-3-buten-1-amine oxalate.
    Molecular formula C12H16N2O4.
    CAS No.: 220662-95-3
    Activity RJR 2403 oxalate activates α4/β2 nAChR EC50 ~ 16 μM1.
    1. Papke, R.L. et al. (2000) J. Neurochem. 75, 204.
    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 Water. Centrifuge all product preparations before use (10000 x 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs RJR 2403 oxalate activates α4/β2 nAChR channels heterologously expressed in Xenopus oocytes.
      Alomone Labs RJR 2403 oxalate activates α4/βnAChR channels heterologously expressed in Xenopus oocytes.
      Brief application of 20 µM RJR-2403 oxalate (#R-115) (arrow) elicits transient inward current in α4/β2 nAChR held at -80 mV.
    References - Scientific background
    1. Changeux, J.P. and Edelstein, S.J. (1998) Neuron 21, 959.
    2. Cordero-Erausquin, M. et al. (2000) Trends Pharmacol. Sci. 21, 211.
    3. Papke, R.L. et al. (2000) J. Neurochem. 75, 204.
    4. Luetje, C.W. and Patrick, J. (1991) J. Neurosci11, 837.
    Scientific background

    Neuronal nAChRs are a larger family of ligand-gated ion channels widely expressed in both the central and the peripheral nervous systems. At least 12 different subunits of nAChRs, including α2-α10, β2-β4, have been identified so far and these subunits form many different sub- types of nAChRs with pentameric structures consisting of homomers or heteromers1. It has been shown that nAChRs are involved in a variety of physiological functions including learning, reinforcement, development, aging and nociception2.

    RJR-2403 [(E)-N-methyl-4-(3-pyridinyl)-3-butene-1-amine or metanicotine] is a potent and effective activator of human α4/β2 receptors with a significant selectivity for this receptor subtype (EC50 value = 16 μm)3. RJR-2403 exhibits potency and selectivity for CNS nAChRs thought to play a role in various CNS disorders3. Functional studies show that RJR-2403 is comparable to nicotine in activating rat thalamic synaptosomes (EC50 = 732 nM for RJR-2403 and EC50 = 591 nM for nicotine)4.

    Target α4/β2 nAChRs
    Last update: 06/11/2022

    RJR 2403 oxalate (#R-115) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information