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Submit ReviewPicrotoxin
Description: GABAA antagonist
Purity: ≥97% (HPLC)
Biological Activity for Picrotoxin
Picrotoxin is a GABAA receptor antagonist; potent CNS stimulant.
Technical Data for Picrotoxin
| M. Wt | 602.59 |
| Formula | C30H34O13 |
| Storage | Store at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 124-87-8 |
| PubChem ID | 6473767 |
| InChI Key | VJKUPQSHOVKBCO-ZYMHLGHZSA-N |
| Smiles | [H][C@@]12OC([C@@](C1(C(C)=C)[H])([C@@]3(C[C@H]4O[C@]45C(O[C@]2([C@]35C)[H])=O)O)[H])=O.[H][C@@]67OC([C@@](C6(C(C)(O)C)[H])([C@@]8(C[C@H]9O[C@]9%10C(O[C@]7([C@]8%10C)[H])=O)O)[H])=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Picrotoxin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 30.13 | 50 with gentle warming | |
| DMSO | 12.05 | 20 |
Preparing Stock Solutions for Picrotoxin
The following data is based on the product molecular weight 602.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.32 mL | 16.6 mL | 33.19 mL |
| 2.5 mM | 0.66 mL | 3.32 mL | 6.64 mL |
| 5 mM | 0.33 mL | 1.66 mL | 3.32 mL |
| 25 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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Product Datasheets for Picrotoxin
References for Picrotoxin
References are publications that support the biological activity of the product.
Dillon et al (1995) Enhancement by GABA of the association rate of picrotoxin and tert-butylbicyclophosphorothionate to the rat cloned α1β2γ2 GABAA receptor subtype. Br.J.Pharmacol. 115 539 PMID: 7582470
Ette et al (1999) Picrotoxin blockade of inverterbrate glutamate-gated chloride channels: subunit dependence and evidence for binding within the pore. J.Neurochem. 72 318 PMID: 9886084
Newland and Cull-Candy (1992) On the mechanism of action of picrotoxin on GABA receptor channels in dissociated sympathetic neurones of the rat. J.Physiol. 447 191 PMID: 1317428
Merck Index 12 7570
If you know of a relevant reference for Picrotoxin, please let us know.
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Keywords: Picrotoxin, Picrotoxin supplier, GABAA, receptor, antagonists, Receptors, picrotin, 1128, Tocris Bioscience
126 Citations for Picrotoxin
Citations are publications that use Tocris products. Selected citations for Picrotoxin include:
Song et al (2019) Altered Behaviors and Impaired Synaptic Function in a Novel Rat Model With a Complete Shank3 Deletion. Front Cell Neurosci 13 111 PMID: 30971895
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Chen et al (2016) Direct modulation of GFAP-expressing glia in the arcuate nucleus bi-directionally regulates feeding. Elife 5 PMID: 27751234
Dobson et al (2015) Caffeine Modulates Vesicle Release and Recovery at Cerebellar Parallel Fibre Terminals, Independently of Calcium and Cyclic AMP Signalling. J Pharmacol Exp Ther 10 e0125974 PMID: 25933382
Arama et al (2015) GABAA receptor activity shapes the formation of inhibitory synapses between developing medium spiny neurons. Physiol Rep 9 290 PMID: 26300728
Quintana et al (2015) Acid-sensing ion channel 1a drives AMPA receptor plasticity following ischaemia and acidosis in hippocampal CA1 neurons. Front Cell Neurosci 593 4373 PMID: 26174503
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Yoon et al (2012) Mind bomb-1 is an essential modulator of long-term memory and synaptic plasticity via the Notch signaling pathway. Mol Brain 5 40 PMID: 23111145
Ermolyuk et al (2012) Independent regulation of basal neurotransmitter release efficacy by variable Ca2+ influx and bouton size at small central synapses. PLoS Biol 10 e1001396 PMID: 23049481
Janssen et al (2012) Neuregulin directly decreases voltage-gated sodium current in hippocampal ErbB4-expressing interneurons. J Neurosci 32 13889 PMID: 23035098
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285 PMID: 22368777
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Bhat et al (2010) Inhibitory role for GABA in autoimmune inflammation. Proc Natl Acad Sci U S A 107 2580 PMID: 20133656
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Lobb et al (2010) A dynamic role for GABA receptors on the firing pattern of midbrain DArgic neurons. J Neurophysiol 104 403 PMID: 20445035
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Kaneko et al (2010) Constitutively active H-ras accelerates multiple forms of plasticity in developing visual cortex. Proc Natl Acad Sci U S A 107 19026 PMID: 20937865
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Cai and Ford (2018) DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate. Cell Rep 25 3148 PMID: 30540946
Sancho and Bloodgood (2018) Functional Distinctions between Spine and Dendritic Synapses Made onto Parvalbumin-Positive Interneurons in Mouse Cortex. Cell Rep 24 2075 PMID: 30134169
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Ho et al (2016) Rapid Ngn2-induction of excitatory neurons from hiPSC-derived neural progenitor cells. Methods 101 113 PMID: 26626326
Bariselli et al (2016) SHANK3 controls maturation of social reward circuits in the VTA. Nat Neurosci 19 926 PMID: 27273769
Li et al (2016) A Cortical Circuit for Sexually Dimorphic Oxytocin-Dependent Anxiety Behaviors. Cell 167 60 PMID: 27641503
Zhang et al (2016) Loss of MeCP2 in cholinergic neurons causes part of RTT-like phenotypes via α7 receptor in hippocampus. Cell Res 26 728 PMID: 27103432
Cheadle and Biederer (2014) Activity-dependent regulation of dendritic complexity by semaphorin 3A through Farp1. J Biol Chem 34 7999 PMID: 24899721
Pandya and Pillai (2014) TrkB interacts with ErbB4 and regulates NRG1-induced NR2B phosphorylation in cortical neurons before synaptogenesis. J Neurosci 12 47 PMID: 25052836
Vashchinkina et al (2014) Neurosteroid Agonist at GABAA receptor induces persistent neuroplasticity in VTA DA neurons. Neuropsychopharmacology 39 727 PMID: 24077066
Williams et al (2014) Excitatory drive onto DArgic neurons in the rostral linear nucleus is enhanced by NE in an α1 adrenergic receptor-dependent manner. Neuropharmacology 86 116 PMID: 25018040
Chen et al (2010) Neurexin-neuroligin cell adhesion complexes contribute to synaptotropic dendritogenesis via growth stabilization mechanisms in vivo. J Neurophysiol 67 967 PMID: 20869594
Purkey et al (2018) AKAP150 Palmitoylation Regulates Synaptic Incorporation of Ca2+-Permeable AMPA Receptors to Control LTP. Cell Rep 25 974 PMID: 30355502
Rhijn et al (2018) Foxp2 loss of function increases striatal direct pathway inhibition via increased GABA release. Brain Struct Funct 223 4211 PMID: 30187194
Wall et al (2018) The Temporal Dynamics of Arc Expression Regulate Cognitive Flexibility. Neuron 98 1124 PMID: 29861284
McKay et al (2018) The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences. Cell Rep 25 841 PMID: 30355491
Dennis et al (2016) Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus. J Neurosci 26 414 PMID: 26472558
Pan et al (2016) Postnatal development of the electrophysiological properties of somatostatin interneurons in the anterior cingulate cortex of mice. Neuron 6 28137 PMID: 27319800
Hnasko et al (2012) Ventral tegmental area glutamate neurons: electrophysiological properties and projections. J Neurosci 32 15076 PMID: 23100428
Paz et al (2011) A new mode of corticothalamic transmission revealed in the Gria4(-/-) model of absence epilepsy. J Biol Chem 14 1167 PMID: 21857658
Mark et al (2011) Delayed postnatal loss of P/Q-type calcium channels recapitulates the absence epilepsy, dyskinesia, and ataxia phenotypes of genomic Cacna1a mutations. J Neurosci 31 4311 PMID: 21411672
Lam et al (2011) Leptin does not directly affect CNS serotonin neurons to influence appetite. Stem Cell Reports 13 584 PMID: 21531340
Lazarevic et al (2011) Extensive remodeling of the presynaptic cytomatrix upon homeostatic adaptation to network activity silencing. Mol Pain 31 10189 PMID: 21752995
Petropoulos et al (2024) Transcription-replication conflicts underlie sensitivity to PARP inhibitors. Nature 628 433 PMID: 38509368
Tozzi et al (2015) Endogenous 17β-OE is required for activity-dependent long-term potentiation in the striatum: interaction with the DArgic system. Front Cell Neurosci 9 192 PMID: 26074768
Eales et al (2014) The MK2/3 cascade regulates AMPAR trafficking and cognitive flexibility. Nat Commun 5 4701 PMID: 25134715
Tani et al (2014) A local glutamate-glutamine cycle sustains synaptic excitatory transmitter release. Neuron 81 888 PMID: 24559677
Easton et al (2014) Genetic elimination of GABAergic neurotransmission reveals two distinct pacemakers for spontaneous waves of activity in the developing mouse cortex. J Neurosci 34 3854 PMID: 24623764
An et al (2014) Neuritin can normalize neural deficits of Alzheimer's disease. Cell Death Dis 5 e1523 PMID: 25393479
Wang et al (2014) SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks. PLoS One 8 e83941 PMID: 24391850
Simon et al (2014) Gap junction networks can generate both ripple-like and fast ripple-like oscillations. Eur J Neurosci 39 46 PMID: 24118191
Xia et al (2014) Regulation of action potential waveforms by axonal GABAA receptors in cortical pyramidal neurons. PLoS One 9 e100968 PMID: 24971996
Mameza et al (2013) SHANK3 gene mutations associated with autism facilitate ligand binding to the Shank3 ankyrin repeat region. J Neurosci 288 26697 PMID: 23897824
Wang et al (2013) Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons. PLoS One 8 e61787 PMID: 23593498
Chanda et al (2013) Neurons generated by direct conversion of fibroblasts reproduce synaptic phenotype caused by autism-associated neuroligin-3 mutation. Cell Commun Signal 110 16622 PMID: 24046374
Brady et al (2013) Moderate prenatal alcohol exposure reduces plasticity and alters NMDA receptor subunit composition in the dentate gyrus. Cell Metab 33 1062 PMID: 23325244
Wang et al (2011) A critical role for GluN2B-containing NMDA receptors in cortical development and function. Neuron 72 789 PMID: 22153375
Higley et al (2011) Cholinergic interneurons mediate fast VGluT3-dependent glutamatergic transmission in the striatum. PLoS One 6 e19155 PMID: 21544206
Parker et al (2011) Attenuating GABA(A) receptor signaling in DA neurons selectively enhances reward learning and alters risk preference in mice. J Neurosci 31 17103 PMID: 22114279
Straub et al (2011) Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1. Nat Neurosci 14 866 PMID: 21623363
Storey et al (2011) Molecular determinants controlling NMDA receptor synaptic incorporation. J Neurosci 31 6311 PMID: 21525271
Etherton et al (2011) An autism-associated point mutation in the neuroligin cytoplasmic tail selectively impairs AMPA receptor-mediated synaptic transmission in hippocampus. EMBO J 30 2908 PMID: 21642956
George et al (2011) A diversity of synaptic filters are created by temporal summation of excitation and inhibition. J Neurosci 31 14721 PMID: 21994388
Li et al (2017) A Critical Role of Presynaptic Cadherin/Catenin/p140Cap Complexes in Stabilizing Spines and Functional Synapses in the Neocortex. Neuron 94 1155 PMID: 28641114
Liu et al (2017) IGF1-Dependent Synaptic Plasticity of Mitral Cells in Olfactory Memory during Social Learning. Neuron 95 106 PMID: 28683263
Ferrante et al (2017) Post-Inhibitory Rebound Spikes in Rat Medial Entorhinal Layer II/III Principal Cells: In Vivo, In Vitro, and Computational Modeling Characterization. Cereb Cortex 27 2111 PMID: 26965902
Sando et al (2017) Assembly of Excitatory Synapses in the Absence of Glutamatergic Neurotransmission. Neuron 94 312 PMID: 28426966
Gioia et al (2017) Ethanol Mediated Inhibition of Synaptic Vesicle Recycling at Amygdala Glutamate Synapses Is Dependent upon Munc13-2. Front Neurosci 11 424 PMID: 28785200
Kash et al (2008) DA enhances fast excitatory synaptic transmission in the extended amygdala by a CRF-R1-dependent process. J Neurosci 28 13856 PMID: 19091975
Manning et al (2008) NMDA receptor blockade with Mem. attenuates white matter injury in a rat model of periventricular leukomalacia. J Biol Chem 28 6670 PMID: 18579741
Soriano et al (2008) Specific targeting of pro-death NMDA receptor signals with differing reliance on the NR2B PDZ ligand. J Neurosci 28 10696 PMID: 18923045
Spoljaric et al (2019) KCC2-Mediated Cl- Extrusion Modulates Spontaneous Hippocampal Network Events in Perinatal Rats and Mice. Cell Rep 26 1073 PMID: 30699338
Yang and Sun (2015) Hierarchical organization of long-range circuits in the olfactory cortices. Cereb Cortex 3 PMID: 26416972
Dobson and Bellamy (2015) Localization of Presynaptic Plasticity Mechanisms Enables Functional Independence of Synaptic and Ectopic Transmission in the Cerebellum. Sci Rep 2015 602356 PMID: 26171253
Chanda et al (2014) Generation of induced neuronal cells by the single reprogramming factor ASCL1. PLoS One 3 282 PMID: 25254342
Beckley et al (2013) Medial prefrontal cortex inversely regulates toluene-induced changes in markers of synaptic plasticity of mesolimbic DA neurons. J Neurosci 33 804 PMID: 23303956
Neuser et al (2013) Region-specific integration of embryonic stem cell-derived neuronal precursors into a pre-existing neuronal circuit. PLoS One 8 e66497 PMID: 23840491
Rehak et al (2013) Low voltage activation of KCa1.1 current by Cav3-KCa1.1 complexes. PLoS One 8 e61844 PMID: 23626738
Hou and Yu (2013) Activity-regulated somatostatin expression reduces dendritic spine density and lowers excitatory synaptic transmission via postsynaptic somatostatin receptor 4. J Biol Chem 288 2501 PMID: 23233668
Li et al (2011) Synergistic activation of DA D1 and TrkB receptors mediate gain control of synaptic plasticity in the basolateral amygdala. PLoS One 6 e26065 PMID: 22022509
Lecrux et al (2011) Pyramidal neurons are "neurogenic hubs" in the neurovascular coupling response to whisker stimulation. J Neurosci 31 9836 PMID: 21734275
Thompson and Perkel (2011) Endocannabinoids mediate synaptic plasticity at glutamatergic synapses on spiny neurons within a basal ganglia nucleus necessary for song learning. J Neurophysiol 105 1159 PMID: 21177997
Nobis et al (2011) β-Adrenergic receptors enhance excitatory transmission in the bed nucleus of the stria terminalis through a corticotrophin-releasing factor receptor-dependent and cocaine-regulated mechanism. Biol Psychiatry 69 1083 PMID: 21334600
Shiratsuchi et al (2009) PropF. inhibits pressure-stimulated macrophage phagocytosis via the GABAA receptor and dysregulation of p130cas phosphorylation. Am J Physiol Cell Physiol 296 C1400 PMID: 19357231
Yeo et al (2009) Novel repression of Kcc2 transcription by REST-RE-1 controls developmental switch in neuronal chloride. Nat Neurosci 29 14652 PMID: 19923298
Dixon et al (2009) PICK1-mediated glutamate receptor subunit 2 (GluR2) trafficking contributes to cell death in oxygen/glucose-deprived hippocampal neurons. J Neurosci 284 14230 PMID: 19321442
Long et al (2009) Nerve Terminal GABAA Receptors Activate Ca2+/Calmodulin-dependent Signaling to Inhibit Voltage-gated Ca2+ Influx and Glutamate Release. J Neurosci 284 8726 PMID: 19141616
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Filter by:
Works as GABA-A receptor antagonist..
By
Anonymous on 06/01/2020
Assay Type: Ex Vivo
Species: Mouse
Picrotoxin stock was prepared in DMSO and diluted with ACSF to 25 micromolar concentration. Bath application of Picrotoxin blocked evoked inhibitory postsynaptic currents in an ex-vivo slice preparation.
Picrotoxin blocks single-channel openings of GABA-A receptor.
By
Anonymous on 07/21/2019
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Hippocampus
20 microM Picrotoxin concentration was used to block GABA-A receptor openings in nucleated cell membrane patches. Full block was achieved in ~30 seconds after application. Picture: GABA-A receptor openings under control conditions (top three traces) and after application of Picrotoxin (bottom trace).
silence GABA activity.
By
Karthik krishnamurthy on 10/26/2018
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: cortical neurons
Used to block GABA activity in 16 day old cortical neurons. Effective at 10 micromolar concentration. Incubated for 30 minutes before measuring bursts.
GABA blocker.
By
Anonymous on 10/02/2018
Assay Type: Ex Vivo
Species: Rat
Used for electrophysiology to block GABA currents. Works as expected
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