(+)-Bicuculline

Catalog # Availability Size / Price Qty
0130/50
(+)-Bicuculline | CAS No. 485-49-4 | GABA-A Receptor Antagonists
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Description: Potent GABAA antagonist

Chemical Name: [R-(R*,S*)]-6-(5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl)furo[3,4-e]-1,3-benzodioxol-8(6H)-one

Product Details
Citations (98)
Supplemental Products
Reviews (1)

Biological Activity

Classical GABAA antagonist.

Methoiodide Salt, Methobromide Salt and Methochloride Salt also available.

Technical Data

Formula:
C20H17NO6
Solubility:
Soluble to 100 mM in DMSO
Storage:
Store the unopened product at 2 - 8 °C. Do not use past expiration date.
CAS No:
485-49-4

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.

Additional Information

Background References

  1. Studies on the neuropharmacological activity of bicuculline and related compounds.
    Olsen et al.
    Brain Res., 1976;102:283
  2. GABA, bicuculline and central inhibition.
    Curtis et al.
    Nature, 1970;226:1222
  3. Intracerebral site of convulsant action of bicuculline.
    Piredda et al.
    Life Sci., 1985;36:1295
  4. Multiplicity of GABAA-benzodiazepine receptors.
    Sieghart et al.
    TiPS, 1989;10:407

Product Datasheets

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Citations for (+)-Bicuculline

The citations listed below are publications that use Tocris products. Selected citations for (+)-Bicuculline include:

98 Citations: Showing 1 - 10

  1. Sonic hedgehog expression in the postnatal brain.
    Authors: Rivell Et al.
    Biol Open  2019;8
  2. Myosin VI Drives Clathrin-Mediated AMPA Receptor Endocytosis to Facilitate Cerebellar Long-Term Depression.
    Authors: Wagner Et al.
    Cell Rep  2019;28:11
  3. Modulation of Functional Connectivity Between DA Neurons of the Rat Ventral Tegmental Area in vitro.
    Authors: Velden Et al.
    Front Integr Neurosci  2019;13:20
  4. AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation.
    Authors: Marinangeli Et al.
    iScience  2018;9:1
  5. Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation.
    Authors: Zhang Et al.
    Neuron  2018;98:918
  6. JIP1-Mediated JNK Activation Negatively Regulates Synaptic Plasticity and Spatial Memory.
    Authors: Morel Et al.
    J Neurosci  2018;38:3708
  7. The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences.
    Authors: McKay Et al.
    Cell Rep  2018;25:841
  8. Impairments of spatial memory in an Alzheimer's disease model via degeneration of hippocampal cholinergic synapses.
    Authors: Zhu Et al.
    Nat Commun  2017;8:1676
  9. δ-subunit containing GABAA receptors modulate respiratory networks.
    Authors: Montandon
    Sci Rep  2017;7(1):18105
  10. The RNA-Binding Protein hnRNP K Mediates the Effect of BDNF on Dendritic mRNA Metabolism and Regulates Synaptic NMDA Receptors in Hippocampal Neurons.
    Authors: Leal Et al.
    Eneuro  2017;4
  11. Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity.
    Authors: Li Et al.
    Cell  2017;168:86
  12. Glycinergic dysfunction in a subpopulation of dorsal horn interneurons in a rat model of neuropathic pain
    Authors: Imlach Et al.
    Scientific Reports  2016;6:37104
  13. Ring finger protein 10 is a novel synaptonuclear messenger encoding activation of NMDA receptors in hippocampus.
    Authors: Dinamarca Et al.
    Elife  2016;5
  14. Identification of small molecules that improve ATP synthesis defects conferred by Leber's hereditary optic neuropathy mutations.
    Authors: Datta Et al.
    Mitochondrion  2016;30:177
  15. γ-Aminobutyric Acid Type A (GABAA) Receptor Subunits Play a Direct Structural Role in Synaptic Contact Formation via Their N-terminal Extracellular Domains.
    Authors: Brown Et al.
    J Biol Chem  2016;291:13926
  16. Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain.
    Authors: Acuña Et al.
    J Clin Invest  2016;126:2547
  17. Tissue plasminogen activator inhibits NMDA-receptor-mediated increases in calcium levels in cultured hippocampal neurons.
    Authors: Robinson Et al.
    Front Cell Neurosci  2015;9:404
  18. Glycine and GABAA receptors mediate tonic and phasic inhibitory processes that contribute to prepulse inhibition in the goldfish startle network.
    Authors: Curtin and Preuss
    Front Neural Circuits  2015;9:12
  19. Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia.
    Authors: Campbell Et al.
    Front Cell Neurosci  2015;8:425
  20. N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity.
    Authors: Lee Et al.
    Mol Brain  2015;8:4
  21. LRP8-Reelin-Regulated Neuronal Enhancer Signature Underlying Learning and Memory Formation.
    Authors: Telese Et al.
    Neuron  2015;86:696
  22. Co-release of glutamate and GABA from single vesicles in GABAergic neurons exogenously expressing VGLUT3.
    Authors: Zimmermann Et al.
    Front Synaptic Neurosci  2015;7:16
  23. Brain ischemia downregulates the neuroprotective GDNF-Ret signaling by a calpain-dependent mechanism in cultured hippocampal neurons.
    Authors: Curcio Et al.
    Cell Death Dis  2015;6:e1645
  24. Wnt signalling tunes neurotransmitter release by directly targeting Synaptotagmin-1.
    Authors: Ciani Et al.
    Nat Commun  2015;6:8302
  25. Subventricular zone neural progenitors reverse TNF-α effects in cortical neurons.
    Authors: Morini Et al.
    Stem Cell Res Ther  2015;6:166
  26. Synaptic structure and function are altered by the neddylation inhibitor MLN4924.
    Authors: Scudder and Patrick
    Mol Cell Neurosci  2015;65:52
  27. Acid-sensing ion channel 1a drives AMPA receptor plasticity following ischaemia and acidosis in hippocampal CA1 neurons.
    Authors: Quintana Et al.
    J Physiol  2015;593:4373
  28. Forebrain deletion of the dystonia protein torsinA causes dystonic-like movements and loss of striatal cholinergic neurons.
    Authors: Pappas Et al.
    Elife  2015;4:e08352
  29. α6-Containing GABAA Receptors Are the Principal Mediators of Inhibitory Synapse Strengthening by Ins in Cerebellar Granule Cells.
    Authors: Accardi Et al.
    J Neurosci  2015;35:9676
  30. Disruption of Fgf13 causes synaptic excitatory-inhibitory imbalance and genetic epilepsy and febrile seizures plus.
    Authors: Puranam Et al.
    J Neurosci  2015;35:8866
  31. Developmental changes in synaptic distribution in arcuate nucleus neurons.
    Authors: Baquero Et al.
    J Neurosci  2015;35:8558
  32. Life extension factor klotho prevents mortality and enhances cognition in hAPP transgenic mice.
    Authors: Dubal Et al.
    J Neurosci  2015;35:2358
  33. Role of parafacial nuclei in control of breathing in adult rats.
    Authors: Huckstepp Et al.
    J Neurosci  2015;35:1052
  34. The reinforcing effects of ethanol within the nucleus accumbens shell involve activation of local GABA and serotonin receptors.
    Authors: Ding Et al.
    J Psychopharmacol  2015;29:725
  35. Soluble epoxide hydrolase inhibitor enhances synaptic neurotransmission and plasticity in mouse prefrontal cortex.
    Authors: Wu Et al.
    J Biomed Sci  2015;22:94
  36. Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus.
    Authors: John Et al.
    Brain Res  2015;1601:15
  37. The effect of BLA GABA(A) receptors in anxiolytic-like effect and aversive memory deficit induced by ACPA.
    Authors: Kangarlu-Haghighi Et al.
    EXCLI J  2015;14:613
  38. MARK/Par1 Kinase Is Activated Downstream of NMDA Receptors through a PKA-Dependent Mechanism.
    Authors: Bernard and Zhang
    PLoS One  2015;10:e0124816
  39. Daily isofl. exposure increases barbiturate insensitivity in medullary respiratory and cortical neurons via expression of η-subunit containing GABA ARs.
    Authors: Hengen Et al.
    PLoS One  2015;10:e0119351
  40. Activation of mGluR2/3 underlies the effects of N-acetylcystein on amygdala-associated autism-like phenotypes in a valproate-induced rat model of autism.
    Authors: Chen Et al.
    Front Behav Neurosci  2014;8:219
  41. Loss of mTOR repressors Tsc1 or Pten has divergent effects on excitatory and inhibitory synaptic transmission in single hippocampal neuron cultures.
    Authors: Weston Et al.
    Front Mol Neurosci  2014;7:1
  42. Imaging intraorganellar Ca2+ at subcellular resolution using CEPIA.
    Authors: Suzuki Et al.
    Nat Commun  2014;5:4153
  43. Mitochondrial reactive oxygen species regulate the strength of inhibitory GABA-mediated synaptic transmission.
    Authors: Accardi Et al.
    Nat Commun  2014;5:3168
  44. Long-term depression-inducing stimuli promote cleavage of the synaptic adhesion molecule NGL-3 through NMDA receptors, matrix metalloproteinases and presenilin/γ-secretase.
    Authors: Lee Et al.
    Philos Trans R Soc Lond B Biol Sci  2014;369:20130158
  45. Phosphorylation of synapsin I by cyclin-dependent kinase-5 sets the ratio between the resting and recycling pools of synaptic vesicles at hippocampal synapses.
    Authors: Verstegen Et al.
    J Neurosci  2014;34:7266
  46. Mutations that disrupt Ca2+-binding activity endow Doc2β with novel functional properties during synaptic transmission.
    Authors: Gaffaney Et al.
    Mol Biol Cell  2014;25:481
  47. CaMKII phosphorylation of neuroligin-1 regulates excitatory synapses.
    Authors: Bemben Et al.
    Nat Neurosci  2014;17:56
  48. Distinct temporal expression of 5-HT(1A) and 5-HT(2A) receptors on cerebellar granule cells in mice.
    Authors: Oostland Et al.
    Cerebellum  2014;13:491
  49. GPR35 activation reduces Ca2+ transients and contributes to the kynurenic acid-dependent reduction of synaptic activity at CA3-CA1 synapses.
    Authors: Berlinguer-Palmini Et al.
    PLoS One  2013;8:e82180
  50. Impaired glutamate recycling and GluN2B-mediated neuronal calcium overload in mice lacking TGF-β1 in the CNS.
    Authors: Koeglsperger Et al.
    Glia  2013;61:985
  51. Synapsin II desynchronizes neurotransmitter release at inhibitory synapses by interacting with presynaptic calcium channels.
    Authors: Medrihan Et al.
    Nat Commun  2013;4:1512
  52. Disrupted Cl(-) homeostasis contributes to reductions in the inhibitory efficacy of D.pam during hyperexcited states.
    Authors: Deeb Et al.
    Eur J Neurosci  2013;38:2453
  53. The Munc13 proteins differentially regulate readily releasable pool dynamics and calcium-dependent recovery at a central synapse.
    Authors: Chen Et al.
    J Neurosci  2013;33:8336
  54. Endoplasmic reticulum-associated degradation controls cell surface expression of γ-aminobutyric acid, type B receptors.
    Authors: Zemoura Et al.
    J Biol Chem  2013;288:34897
  55. Activity-regulated somatostatin expression reduces dendritic spine density and lowers excitatory synaptic transmission via postsynaptic somatostatin receptor 4.
    Authors: Hou and Yu
    J Biol Chem  2013;288:2501
  56. Long-term potentiation of excitatory synaptic strength in spinothalamic tract neurons of the rat spinal cord.
    Authors: Hur and Park
    Korean J Physiol Pharmacol  2013;17:553
  57. Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity.
    Authors: Korb Et al.
    Nat Neurosci  2013;16:874
  58. Plasticity-related gene 3 promotes neurite shaft protrusion.
    Authors: Velmans Et al.
    BMC Neurosci  2013;14:36
  59. Synaptic and extrasynaptic transmission of kidney-related neurons in the rostral ventrolateral medulla.
    Authors: Gao and Derbenev
    J Neurophysiol  2013;110:2637
  60. Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons.
    Authors: Kaufman Et al.
    J Neurosci  2012;32:3992
  61. Raf kinase inhibitory protein is required for cerebellar long-term synaptic depression by mediating PKC-dependent MAPK activation.
    Authors: Yamamoto Et al.
    J Neurosci  2012;32:14254
  62. Multiple roles for mammalian target of rapamycin signaling in both glutamatergic and GABAergic synaptic transmission.
    Authors: Weston Et al.
    J Neurosci  2012;32:11441
  63. Essential role of brain-derived neurotrophic factor in the regulation of serotonin transmission in the basolateral amygdala.
    Authors: Daftary Et al.
    Neuroscience  2012;224:125
  64. Increased bursting glutamatergic neurotransmission in an auditory forebrain area of the zebra finch (Taenopygia guttata) induced by auditory stimulation.
    Authors: Dagostin Et al.
    J Comp Physiol A Neuroethol Sens Neural Behav Phys  2012;198:705
  65. Uncoupling the roles of synaptotagmin I during endo- and exocytosis of synaptic vesicles.
    Authors: Yao Et al.
    Nat Neurosci  2012;15:243
  66. Basolateral amygdala inactivation impairs learning-induced long-term potentiation in the cerebellar cortex.
    Authors: Zhu Et al.
    PLoS One  2011;6:e16673
  67. Sleep-deprivation regulates α-2 adrenergic responses of rat hypocretin/orexin neurons.
    Authors: Uschakov Et al.
    PLoS One  2011;6:e16672
  68. Potentiating action of PropF. at GABAA receptors of retinal bipolar cells.
    Authors: Yue Et al.
    Invest Ophthalmol Vis Sci  2011;52:2497
  69. Positive feedback regulation between γ-aminobutyric acid type A (GABA(A)) receptor signaling and brain-derived neurotrophic factor (BDNF) release in developing neurons.
    Authors: Porcher Et al.
    J Biol Chem  2011;286:21667
  70. Rapid brain-derived neurotrophic factor-dependent sequestration of amygdala and hippocampal GABA(A) receptors via different tyrosine receptor kinase B-mediated phosphorylation pathways.
    Authors: Mou Et al.
    Neuroscience  2011;176:72
  71. Peripheral calcium-permeable AMPA receptors regulate chronic inflammatory pain in mice.
    Authors: Gangadharan Et al.
    J Clin Invest  2011;121:1608
  72. SV2 mediates entry of tetanus neurotoxin into central neurons.
    Authors: Yeh Et al.
    PLoS Pathog  2010;6:e1001207
  73. Melatonin potentiates glycine currents through a PLC/PKC signalling pathway in rat retinal ganglion cells.
    Authors: Zhao Et al.
    J Physiol  2010;588:2605
  74. Selected SALM (synaptic adhesion-like molecule) family proteins regulate synapse formation.
    Authors: Mah Et al.
    J Neurosci  2010;30:5559
  75. OE acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism.
    Authors: Smejkalova and Woolley
    J Neurosci  2010;30:16137
  76. Cannabinoids excite circadian clock neurons.
    Authors: Acuna-Goycolea Et al.
    J Neurosci  2010;30:10061
  77. Reduction in synaptic GABA release contributes to target-selective elevation of PVN neuronal activity in rats with myocardial infarction.
    Authors: Han Et al.
    Am J Physiol Regul Integr Comp Physiol  2010;299:R129
  78. Imaging activity-dependent regulation of neurexin-neuroligin interactions using trans-synaptic enzymatic biotinylation.
    Authors: Thyagarajan and Ting
    Cell  2010;143:456
  79. Characterization of engineered channelrhodopsin variants with improved properties and kinetics.
    Authors: Lin Et al.
    Biophys J  2009;96:1803
  80. Synaptotagmin has an essential function in synaptic vesicle positioning for synchronous release in addition to its role as a calcium sensor.
    Authors: Young and Neher
    Neuron  2009;63:482
  81. Novel repression of Kcc2 transcription by REST-RE-1 controls developmental switch in neuronal chloride.
    Authors: Yeo Et al.
    J Neurosci  2009;29:14652
  82. Tamoxifen mediated estrogen receptor activation protects against early impairment of hippocampal neuron excitability in an oxygen/glucose deprivation brain slice ischemia model.
    Authors: Zhang Et al.
    Brain Res  2009;1247:196
  83. Postsynaptic glutamate receptor δ family contributes to presynaptic terminal differentiation and establishment of synaptic transmission.
    Authors: Kuroyanagi Et al.
    Proc Natl Acad Sci U S A  2009;106:4912
  84. Histone H2AX-dependent GABA(A) receptor regulation of stem cell proliferation.
    Authors: Andäng Et al.
    Nature  2008;451:460
  85. Glutamatergic transmission is sustained at a later period of development of medial nucleus of the trapezoid body-lateral superior olive synapses in circling mice.
    Authors: Hong Et al.
    J Neurosci  2008;28:13003
  86. Specific targeting of pro-death NMDA receptor signals with differing reliance on the NR2B PDZ ligand.
    Authors: Soriano Et al.
    J Neurosci  2008;28:10696
  87. Resveratrol attenuates early pyramidal neuron excitability impairment and death in acute rat hippocampal slices caused by oxygen-glucose deprivation.
    Authors: Zhang Et al.
    Exp Neurol  2008;212:44
  88. Transient allodynia pain models in mice for early assessment of analgesic activity.
    Authors: Gil Et al.
    Br J Pharmacol  2008;153:769
  89. Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons.
    Authors: Brager and Johnston
    J Neurosci  2007;27:13926
  90. Regulated expression of HCN channels and cAMP levels shape the properties of the h current in developing rat hippocampus.
    Authors: Surges Et al.
    Eur J Neurosci  2006;24:94
  91. A nitric oxide signaling pathway controls CREB-mediated gene expression in neurons.
    Authors: Riccio Et al.
    Mol Cell  2006;21:283
  92. Glutamatergic regulation of the p70S6 kinase in primary mouse neurons.
    Authors: Lenz and Avruch
    J Biol Chem  2005;280:38121
  93. Distinct γ2 subunit domains mediate clustering and synaptic function of postsynaptic GABAA receptors and gephyrin.
    Authors: Alldred Et al.
    J Neurosci  2005;25:594
  94. PropF. suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels.
    Authors: Ying and Goldstein
    Mol Pain  2005;1:2
  95. Endocannabinoids regulate interneuron migration and morphogenesis by transactivating the TrkB receptor.
    Authors: Berghuis Et al.
    Proc Natl Acad Sci U S A  2005;102:19115
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Use of BIC as a selective GABA-A receptor antagonist
By Anonymous on 05/20/2019
Species: Rat

We have used (+)-Bicuculline (BIC) as a control tool to make sure that only GABA-A receptors are active under perfusion with given set of neuroreceptor antagonists.Being applied at membrane patches excised from cerebellar granule cell, 10 microM GABA triggered clear single-channel openings of GABA-A receptors. However, 100 microM BIC added together with GABA completely suppressed all single-channel activity, thus proving absence of other receptor types.

PMID: 23447601

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