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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.
    Structure
    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.
    References-Activity
    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: 12/08/2021

    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