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Muscimol

Agarin, Pantherine

A Potent Agonist of GABA(A) Receptor and a Partial Agonist of GABA(A) ρ Receptor

Cat #: M-241
Alternative Name Agarin, Pantherine
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 114.1
    Purity: >97% (HPLC)
    Effective concentration 0.01-1 µM.
    Structure
    Chemical name 5-(aminomethyl)-1,2-oxazol-3-one.
    Molecular formula C4H6N2O2.
    CAS No.: 2763-96-4
    PubChem CID 4266
    Activity Muscimol is a potent GABAA receptor agonist (EC50 of 0.92, 0.62 and 0.20 µM on α1β3γ2, α4β3γ2 and α4β3δ, 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 +4°C.
    Solubility Soluble 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 Muscimol activates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs Muscimol 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 (#M-241) while membrane potential was held at -60mV.
    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: 25/07/2021

    Muscimol (#M-241) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

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