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Picrotoxin

Cocculin, Picrotin, Picrotoxinin

An Antagonist of GABA(A), Glycine, and 5-HT3 Receptors

Cat #: P-325
Alternative Name Cocculin, Picrotin, Picrotoxinin
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Anamirta cocculus.
    Source Natural
    MW: 602.58
    Purity: >99% (HPLC)
    Effective concentration 1-100 µM.
    Structure
    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.
    References-Activity
    1. Dillon, G.H. et al. (1995) Br. J. Pharmacol. 115, 539.
    2. Wang, D.S. et al. (2006) J. Biol. Chem. 281, 3841.
    3. Das, P. and Dillon, G.H. (2005) J. Pharmacol. Exp. Ther. 314, 320.
    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.
    Our bioassay
    • Alomone Labs Picrotoxin inhibits GABA(A) receptors expressed in Xenopus oocytes.
      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
    1. Wang, D.S. et al. (2006) J. Biol. Chem. 281, 3841.
    2. Das, P. and Dillon, G.H. (2005) J. Pharmacol. Exp. Ther. 314, 320.
    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
    Lyophilized Powder
    Last update: 06/11/2022

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

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    For research purposes only, not for human use
    Shipping and Ordering information

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