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AA 29504

A Positive Modulator of GABA(A) Receptors
Cat #: A-370
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 327.43
    Purity: >98%
    Effective concentration 1-100 µM.
    Structure
    Chemical name Ethyl N-[2-amino-4-[(2,4,6-trimethylphenyl)methylamino]phenyl]carbamate.
    Molecular formula C19H25N3O2.
    CAS No.: 945828-50-2.
    PubChem CID 23188887
    Activity AA 29504 is a positive allosteric modulator of GABA(A) receptors, reducing the EC50 of GABA and gaboxadol at the α4β3δ and α1β3γ2S receptors in Xenopus oocytes at over 1 µM. AA 29504, a retigabine analogue, also exhibits some agonistic activity on KCNQ channels (EC50=9.6-13.5 µM)1.
    References-Activity
    1. Hoestgaard-Jensen, K. et al. (2010) Neuropharmacology 58, 702.
    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 +4°C.
    Solubility Soluble in DMSO. Centrifuge all product preparations before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs AA 29504 activates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs AA 29504 activates GABA(A) receptors expressed in Xenopus oocytes.
      Time course of GABA(A) α1/β2 currents, reversibly activated in a concentration dependent manner by 1 µM, 5 µM and 25 µM AA 29504 (#A-370), while membrane potential was held at -60mV.
    References - Scientific background
    1. Hoestgaard-Jensen, K. et al. (2010) Neuropharmacology 58, 702.
    2. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    3. Iqbal, F. et al. (2011) Bioorg. Med. Chem. Lett. 21, 4252.
    Scientific background

    AA 29504, a close analogue of retigabine (KCNQ channel opener), acts as a positive allosteric modulator of GABA(A) receptors. A study in adult rats shows that systemic administration of AA 29504 produces anxiolytic effects and reduces motor coordination1.

    AA 29504 decreases the EC50 value of GABA at the GABA (A) receptors in Xenopus oocytes at over 1 µM. The compound also exhibits agonistic activity on KCNQ channels and demonstrates EC50 values of 9.6-13.5 µM1.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. These receptors mediate GABA action, a major inhibitory neurotransmitter, throughout the central nervous system (CNS). They play an important role in inhibiting cell excitation in the CNS. The GABA(A) receptor is considered to be a major target of antiseizure drugs2,3.

    Target GABA(A) receptors
    Last update: 23/08/2020

    AA 29504 (#A-370) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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