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(S)-ATPO

CHEMBL5664840

An Antagonist of AMPA/Kainate Receptors

Cat #: A-330
Alternative Name CHEMBL5664840
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 322.25
    Purity: >95%
    Effective concentration 0.1-500 µM.
    Structure
    Chemical name (2S)-2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-1,2-oxazol-4-yl]propanoic acid.
    Molecular formula C11H19N2O7P.
    CAS No.: 252930-37-3
    PubChem CID 447249
    Activity An active enantiomer of ATPO, an antagonist of GluR1-4 and a partial agonist of GluR5. (S)-ATPO antagonized AMPA-induced depolarization in the cortical wedge preparation with (IC50 =15 μM)1.
    References-Activity
    1. Møller, E.H. et al. (1999) Chirality 11, 752.
    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 Up to 100 mM in 1eq NaOH. Centrifuge all products before reconstitution (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C. It is recommended to aliquot reconstituted stock solutions.
    Our bioassay
    • Alomone Labs (S)-ATPO inhibits GluA1 receptors expressed in Xenopus oocytes. 
      Alomone Labs (S)-ATPO inhibits GluA1 receptors expressed in Xenopus oocytes. 
      Time course of GluA1 currents, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 10 µM and 100 µM (S)-ATPO (#A-330), as indicated (bars), at a holding potential of -60 mV.
    References - Scientific background
    1. Møller, E.H. et al. (1999) Chirality 11, 752.
    2. Guntupalli, S. et al. (2016) Neural. Plast. 2016, 3204519.
    3. Niu, L. et al. (2015) Acta. Pharm. Sin. B. 5, 500.
    Scientific background

    ATPO, a phosphono amino acid, is a structural hybrid between the NMDA antagonist (RS)-2-amino-7-phosphonoheptanoic acid (AP7) and the AMPA and GluR5 agonist, (RS)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl) propionic acid (ATPA).

    (S)-ATPO acts as a potent and selective AMPA and kainate receptor antagonist. ATPO has the ability to competitively reduce peak responses evoked by semi-rapid applications of AMPA1. It antagonizes AMPA-induced depolarization in the cortical wedge preparation with an IC50 value of 15 µM1.

    AMPA receptors are the principal glutamate receptors that mediate fast excitatory neurotransmission. This function is essential for synaptic plasticity and cellular correlate of learning and memory. Antagonists of AMPA receptors are good drug candidates for potential treatment of several neurological disorders such as epilepsy, stroke and amyotrophic lateral sclerosis (ALS)2,3.

    Target AMPA/Kainate receptors
    Lyophilized Powder
    Last update: 02/01/2022

    (S)-ATPO (#A-330) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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