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RS 56812 hydrochloride

A Potent and Selective 5-HT3 Receptor Agonist

Cat #: R-130
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 347.14
    Purity: >96%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name (R)-N-(1-Azabicyclo[2.2.2]oct-3-yl)-2-(1-methyl-1H-indol-3-yl)-2-(1-methyl-1H-indol-3-yl)-2-oxoacetamide hydrochloride.
    Molecular formula C18H22ClN3O2.
    CAS No.: 143137-35-3
    Activity RS 56812 is a highly potent and selective 5-HT3 partial agonist1.
    References-Activity
    1. Clark, R.D. et al. (1995) Bioorg. Med. Chem. Lett. 5, 1853.
    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 100 mM in water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs RS 56812 hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs RS 56812 hydrochloride activates 5-HT3A receptors expressed in HEK 293T cells. 
      Currents were elicited by 1, 10 or 100 nM RS 56812 hydrochloride (#R-130), as indicated. The currents that were elicited were comparable in amplitude to the cell’s response to 10 µM 5-HT (not shown here).
    References - Scientific background
    1. Van Hooft, J.A. and Vijverberg, H.P. (1997) Eur. J. Pharmacol. 322, 229.
    2. Terry, A.V. Jr et al. (1996) Neuroreport 8, 49.
    Scientific background

    RS 56812 hydrochloride is a highly potent and selective 5-HT3 partial agonist with an EC50 value of 18 nM. It has been shown to bind to 5-HT3 receptors with high affinity. It has the ability to induce the von Bezold-jarisch reflex and to depolarize the rat vagus nerve1.

    The affinity of RS 56812 is comparable to that of other potent full agonists. RS 56812 is thus a valuable tool for investigating the agonist interaction with the 5-HT3 receptor in electrophysiological and radioligand binding studies1.

    RS 56812 exists in the R and S isomeric forms. It has been shown to improve performance in memory tests conducted on monkeys. It appears that the R isomer is more active and seems to produce more systematic and reproducible improvement in memory. RS 56812 is suggested to have a therapeutic potential in disorders involving cognitive decline2.

    Target Serotonin-gated channels
    Last update: 25/04/2021

    RS 56812 hydrochloride (#R-130) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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