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Product overview

  • Name
  • 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
  • Biological action
  • Purity
  • 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

  • Citations



  • Molecular Weight
  • Chemical structure
    Picrotoxin  [124-87-8]
  • Molecular Formula
  • CAS Number
  • PubChem identifier
  • InChi
  • InChiKey
  • MDL number


  • 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)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

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
Our products in action
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
  • Serotonin 2B receptors in mesoaccumbens dopamine pathway regulate cocaine responses

    Doly et al(2017) J Neurosci DOI: : 1354-17
    PubMedID: 28935766
  • Positive regulation of raphe serotonin neurons by serotonin 2B receptors.

    Belmer et al (2018) Neuropsychopharmacology doi: 10.1038/s41386-018-0013-0. : [Epub ahead of print]
    PubMedID: 29453444
  • 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
  • KCC2 regulates neuronal excitability and hippocampal activity via interaction with Task-3 channels

    Poncer et al (2018) bioRxiv doi: :
  • 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
  • A disinhibitory mechanism biases Drosophila innate light preference.

    Zhao et al (2019) Nat Commun 10(1) : 124
    PubMedID: 30631066
  • Synapse-specific Opioid Modulation of Thalamo-cortico-striatal Circuits

    Birdsong et al (2019) bioRxiv :
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Reviews & Product Guides


  • Verified customer

    Reasonable price and it works as it should.
  • summary

    Good. I ordered my chemical to Hello Bio I am too satisfied by their product n got 15% discount also on my first order thank you Hello Bio team.
  • Verified customer, Hamdard University

    I have use this chemical purchase from Hello Bio for my thesis work. I was satisfied by their product.
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