Picrotoxin

Cocculin, Picrotin, Picrotoxinin
An Antagonist of GABA(A), Glycine, and 5-HT3 Receptors
    Cat #: P-325
    Sizes: 500 mg, 1 g, 5 g, 10 g
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Origin Anamirta cocculus.
    Source: Natural
    MW: 602.58 Da.
    Purity >99%.
    Effective concentration 1-100 µM.
    Structure
    Molecular formula C15H18O7·C15H16O6.
    CAS number 124-87-8.
    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.
    Storage before reconstitution Product before reconstitution should be stored at +4°C.
    Reconstitution Soluble in DMSO and ethanol. Centrifuge before use (10000 x g, 5 min).
    Storage after reconstitution Up to three months at -20°C.
    Our bioassay
    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
    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.
    Target: GABA(A), Glycine, 5-HT3 receptors
    Last update: 16/01/2018

    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.

    Alomone Labs is pleased to offer Picrotoxin (#P-325).

    For research purposes only, not for human use