Product overview

  • Name
    Picrotoxin
  • Short description
    Non-competitive GABAA receptor antagonist
  • Biological description
    Non-competitive GABAA receptor antagonist. Also a glycine receptor inhibitor (IC50 = 2.7 µM). Acts as a convulsant and CNS stimulant. Active in vivo.
  • Alternative names
    PTX
  • Biological action
    Antagonist
  • Purity
    >98%
  • Customer comments

    Getting on well with DHPG & picrotoxin – they do what they’re supposed to! Professor Bruno Frenguelli, University of Warwick, UK

  • Our products in action

Images

Properties

  • Molecular Weight
    602.59
  • Chemical structure
    Picrotoxin  [124-87-8]
  • Molecular Formula
    C30H34O13
  • CAS Number
    124-87-8
  • PubChem identifier
    518601
  • SMILES
    CC(=C)C1C2C3C4(C(C1C(=O)O2)(CC5C4(O5)C(=O)O3)O)C.CC12C3C4C(C(C1(CC5C2(O5)C(=O)O3)O)C(=O)O4)C(C)(C)O
  • InChi
    InChI=1S/C15H18O7.C15H16O6/c1-12(2,18)6-7-10(16)20-8(6)9-13(3)14(7,19)4-5-15(13,22-5)11(17)21-9;1-5(2)7-8-11(16)19-9(7)10-13(3)14(8,18)4-6-15(13,21-6)12(17)20-10/h5-9,18-19H,4H2,1-3H3;6-10,18H,1,4H2,2-3H3
  • InChiKey
    VJKUPQSHOVKBCO-UHFFFAOYSA-N
  • MDL number
    MFCD00074824

Applications

  • Application notes

    The GABAA receptor antagonist Picrotoxin is commonly used to reduce the levels inhibition by blocking the actions of the neurotransmitter GABA. Picrotoxin from Hello Bio reduces both spontaneous inhibitory post synaptic currents (IPSC) and evoked IPSCs. It was effective at concentrations of 10μM, with complete receptor blockade at 100μM. For assay protocol, see #Protocol 1 in Application Notes below

     

    #Protocol 1: Evoked and spontaneous inhibitory post synaptic currents (IPSCs)

    • Whole cell voltage clamp recordings were obtained from layer V neurons of the mouse prelimbic cortex brain slice.
    • A stimulating electrode was placed in layers II/III and IPSCs were evoked by a single square (150 μs) pulse every 10 sec at a stimulus intensity that gave a reliable IPSC.
    • IPSCs were evoked at a range of neuron holding voltages to measure the reversal potential of the current to ensure it was GABAergic.
    • Neurons were held at 0mV and IPSCs continuously stimulated and recorded in response to 5 min applications of varying concentrations of Gabazine until complete receptor inhibition.
    • Spontaneous IPSCs were recorded before and after addition of Gabazine by holding the neuron at 0mV and recording for 10 sec.
    • All recordings for IPSCs were made in the presence of AMPAR antagonists.

Storing and Using Your Product

  • Storage instructions
    Room temperature
  • Solubility overview
    Soluble in DMSO (100mM) and in ethanol (50mM, gentle warming)

References for Picrotoxin

  • Picrotoxin-like channel blockers of GABAA receptors.

    Olsen RW (2006) Proc Natl Acad Sci U S A 103(16) : 6081-2.
    PubMedID: 16606858
  • Mechanisms for picrotoxin block of alpha2 homomeric glycine receptors.

    Wang DS et al (2006) J Biol Chem 281(7) : 3841-55.
    PubMedID: 16344549
  • Picrotoxin blockade of invertebrate glutamate-gated chloride channels: subunit dependence and evidence for binding within the pore.

    Etter A et al (1999) J Neurochem 72(1) : 318-26.
    PubMedID: 9886084
The following papers have cited the use of Picrotoxin (HB0506) from Hello Bio. If you have published a paper using this product, and it is not shown here, then please tell us! We will send you a free gift as a thank you!
  • mGluR-LTD at Excitatory and Inhibitory Synapses in the Lateral Habenula Tunes Neuronal Output.

    Valentinova and Mameli(2016) Cell Rep 16(9) : 2298-307
    PubMedID: 27545888
  • PAR1 activation induces rapid changes in glutamate uptake and astrocyte morphology.

    Sweeny et al (2017) Sci Rep. 7 : 43606
    PubMedID: 28256580

Reviews & Product Guides

Reviews

  • Verified customer, University of Bristol

    Our lab has used Hello Bio Picrotoxin to block GABAA receptors.