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Muscimol hydrobromide

Agarin hydrobromide
A Potent Agonist of GABA(A) Receptor and a Partial Agonist of GABA(A) ρ Receptor
Cat #: M-240
Alternative Name Agarin hydrobromide
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 195.01
    Purity: >96% (HPLC)
    Effective concentration 0.01-1 µM.
    Structure
    Chemical name 5-(aminomethyl)-1,2-oxazol-3-one; hydrobromide.
    Molecular formula C4H7BrN2O2.
    CAS No.: 18174-72-6.
    PubChem CID 205536
    Activity Muscimol is a potent GABAA receptor agonist (EC50 of 0.92, 0.62 and 0.20 µM on α1/β3/γ2, α4/β3/γ2 and α4/β3/δ, respectively)1. It is also a partial agonist at GABAA-ρ receptor (EC50 of 3 µM on human homopentameric ρ1 receptor)2.
    References-Activity
    1. Mortensen, M. et al. (2010) J. Physiol. 588, 1251.
    2. Wang, J. et al. (2007) J. Biol. Chem. 282, 26210.
    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 200 mM in H2O. 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 Muscimol hydrobromide activates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs Muscimol hydrobromide activates GABA(A) receptors expressed in Xenopus oocytes.
      Time course of GABA(A) α1/β2 currents, reversibly activated in a concentration dependent manner by 0.01 µM, 0.1 µM and 1 µM Muscimol hydrobromide (#M-240) while membrane potential was held at -60 mV.
    References - Scientific background
    1. Hosseini, M. et al. (2014) Emerg. (Tehran) 2, 151.
    2. Mortensen, M. et al. (2010) J. Physiol. 588, 1251.
    3. Nohria, V. and Giller, E. (2007) Neurotherapeutics 4, 102.
    Scientific background

    Muscimol (also known as Agarin) is a potent and selective GABA(A) receptor agonist and a partial agonist of GABA(C) receptor1,2. It activates the receptors through a structural transition from the closed to the open state. Muscimol demonstrates potency with EC50 values of 0.92 µM on α1/β3/γ2 receptor and 0.20 µM on α4/β/3δ receptor2.

    The compound is extracted from the mushroom Amanita muscaria as a psychotropic drug and is being used as a local anesthetic drug. Studies have shown the effectiveness of muscimol for reduction of neuropathic pain symptoms1.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate the actions of GABA, a major inhibitory neurotransmitter, in the central nervous system. The GABA(A) receptor is considered to be a major target of antiseizure drugs1,3.

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

    Muscimol hydrobromide (#M-240) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

    Citations

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