Picrotoxin

Cocculin, Picrotin, Picrotoxinin
An Antagonist of GABA(A), Glycine, and 5-HT3 Receptors
    Cat #: P-325
    Alternative Name Cocculin, Picrotin, Picrotoxinin
  • Lyophilized Powder
  • Bioassay Tested
  • Origin Anamirta cocculus.
    Source Natural
    MW: 602.58
    Purity: >99% (HPLC)
    Effective concentration 1-100 µM.
      • Picrotoxin
    Molecular formula C15H18O7·C15H16O6.
    CAS No.: 124-87-8.
    PubChem CID 6473767
    Activity Picrotoxin, an equimolar mixture of picrotoxinin and picrotin, is a non-competitive antagonist of the GABA(A) receptors (IC50 = 2.4 µM – 17 µM)1, an antagonist of glycine receptors (IC50 = 2.7 µM – 6.4 µM)2 and of 5-HT3 receptors (IC50 = 41.2 µM)3.
    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 and ethanol. Centrifuge before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
      • Picrotoxin
        Alomone Labs Picrotoxin inhibits GABA(A) receptors expressed in Xenopus oocytes.
        Representative time course of GABA(A) α1/β2 current, activated by a continuous application (top dotted line) of 0.1 µM γ-aminobutyric acid (#G-110), and inhibited by 10 µM Picrotoxin (#P-325), as indicated (bar), at a holding potential of -60 mV.
    References - Scientific background
      • Picrotoxin (PTX) is a plant-derived alkaloid that originally showed to be a noncompetitive antagonist of GABA(A) receptors. Later it was discovered that picrotoxin inhibits other anion-selective ligand-gated anion channels including glycine and 5-hydroxytryptamine type 3 (5-HT3) receptors. Inhibition by picrotoxin is likely in a noncompetitive, use-facilitated manner through binding to the channel pore of the receptor1,2.

        5-HT3 receptor is a member of the cys-loop superfamily of ligand-gated ion channels (LGICs) that includes nicotinic acetylcholine receptors, GABAA, glycine receptors, glutamate and purinergic receptors1,2.

    Target GABA(A), Glycine, 5-HT3 receptors
    Last update: 22/08/2019

    Picrotoxin (#P-325) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use