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SR 57227A

SR 57227 hydrochloride

A Potent and Selective Agonist of 5-HT3 Receptors

Cat #: S-155
Alternative Name SR 57227 hydrochloride
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 248.15
    Purity: >96%
    Effective concentration 100 nM - 100 µM.
    Structure
    Chemical name 1-(6-chloropyridin-2-yl)piperidin-4-amine hydrochloride.
    Molecular formula C10H15Cl2N3.
    CAS No.: 77145-61-0
    Activity SR 57227A is a high affinity, selective 5-HT3 receptor agonist, active in vivo and CNS penetrant1.
    References-Activity
    1. Bachy, A. et al. (1993) Eur. J. Pharmacol. 237, 299.
    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 50 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 SR 57227A activates 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs SR 57227A activates 5-HT3A receptors expressed in HEK 293T cells. 
      Currents were elicited by 1 or 10 µM SR 57227A (#S-155), as indicated.  The currents that were elicited were comparable in amplitude to the cells responses to 10 µM 5-HT (not shown here).
    References - Scientific background
    1. Bachy, A. et al. (1993) Eur. J. Pharmacol. 237, 299.
    2. Guertin, P.A. and Steuer, I. (2005) J. Neurophysiol. 94, 3397.
    3. Poncelet, M. et al. (1995) J. Neural Transm. Gen. Sect. 102, 83.
    Scientific background

    SR 57227A is a compound with high affinity and selectivity for activating 5-HT3 receptors. It acts as an agonist for peripheral and central 5-HT3 receptors, both in vitro and in vivo, with IC50 values between 2.8 and 250 nM with no affinity for other subtypes of 5-HT.

    SD 57227A has the ability to cross the blood brain barrier, unlike many 5-HT3 receptors. Thus, SR 57227A can be used as a useful tool for characterizing the neuropharmacological effects produced by the stimulation of 5-HT3 receptors1.

    Some findings show that administration of SR 57227A can acutely induce and trigger movements and motor response in the hind limbs of adult paraplegic mice2.

    Additional findings indicate that SR 57227A exhibits antidepressant-like activity in rodent and decrease isolation induced aggressive behavior3.

    Target Serotonin-gated channels
    Lyophilized Powder
    Last update: 06/11/2022

    SR 57227A (#S-155) is a highly pure, synthetic, and biologically active compound.

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

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