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Technical documents: SDS CoA Datasheet

Product overview

Name Picrotoxin
Alternative names PTX
Purity >98%
Customer comments

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

Reasonable price and good working! Verified customer, Seoul National University

Description Non-competitive GABAA receptor antagonist
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Picrotoxin inhibition GABAA receptor IPSCs
Picrotoxin: Scientist Approved

Biological Data

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.
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.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in DMSO (100mM) and in ethanol (50mM, gentle warming)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.



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Chemical Data

Purity >98%
Molecular Weight 602.59
Chemical structure Picrotoxin  [124-87-8] Chemical Structure
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
MDL number MFCD00074824

References for Picrotoxin

References are publications that support the biological activity of the product
  • Picrotoxin-like channel blockers of GABAA receptors.

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

    Wang DS et al (2006) J Biol Chem 281(7) : 3841-55.
  • 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.

3 Item(s)

These publications cite the use of Picrotoxin purchased from Hello Bio:
  • Second-hit mosaic mutation in mTORC1 repressor DEPDC5 causes focal cortical dysplasia-associated epilepsy.

    Ribierre et al (2018) J Clin Invest. 128(6) : 2452-2458
    PubMedID: 29708508
  • The Probability of Neurotransmitter Release Governs AMPA Receptor Trafficking via Activity-Dependent Regulation of mGluR1 Surface Expression.

    Sanderson et al (2018) Cell Rep. 25(13) : 3631-3646
    PubMedID: 30590038
  • Noradrenaline Modulates the Membrane Potential and Holding Current of Medial Prefrontal Cortex Pyramidal Neurons via β1-Adrenergic Receptors and HCN Channels.

    Grzelka et al (2017) Front Cell Neurosci. 11:341 : 2
    PubMedID: 29209170
  • PAR1 activation induces rapid changes in glutamate uptake and astrocyte morphology.

    Sweeny et al (2017) Sci Rep. 7 : 43606
    PubMedID: 28256580
  • Serotonin 2B receptors in mesoaccumbens dopamine pathway regulate cocaine responses

    Doly et al (2017) J Neurosci DOI: https://doi.org/10.1523/JNEUROSCI : 1354-17
    PubMedID: 28935766

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