Catalog Number: 0130
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
Biological Activity
Classical GABAA antagonist.

Methoiodide Salt, Methobromide Salt and Methochloride Salt also available.

Technical Data
  • M.Wt:
    367.36
  • Formula:
    C20H17NO6
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    485-49-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Other Product-Specific Information:
Background References

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

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

67 Citations: Showing 1 - 10
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  1. 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?
  2. Ring finger protein 10 is a novel synaptonuclear messenger encoding activation of NMDA receptors in hippocampus.
    Authors: Dinamarca Et al.
    Elife 2016;5
  3. 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
  4. 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
  5. 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
  6. N-methyl-D-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
  7. LRP8-Reelin-Regulated Neuronal Enhancer Signature Underlying Learning and Memory Formation.
    Authors: Telese Et al.
    Neuron 2015;86:696
  8. 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
  9. 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
  10. Wnt signalling tunes neurotransmitter release by directly targeting Synaptotagmin-1.
    Authors: Ciani Et al.
    Nat Commun 2015;6:8302
  11. Subventricular zone neural progenitors reverse TNF-α effects in cortical neurons.
    Authors: Morini Et al.
    Stem Cell Res Ther 2015;6:166
  12. 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
  13. 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
  14. Disruption of Fgf13 causes synaptic excitatory-inhibitory imbalance and genetic epilepsy and febrile seizures plus.
    Authors: Puranam Et al.
    J Neurosci 2015;35:8866
  15. Developmental changes in synaptic distribution in arcuate nucleus neurons.
    Authors: Baquero Et al.
    J Neurosci 2015;35:8558
  16. Life extension factor klotho prevents mortality and enhances cognition in hAPP transgenic mice.
    Authors: Dubal Et al.
    J Neurosci 2015;35:2358
  17. Role of parafacial nuclei in control of breathing in adult rats.
    Authors: Huckstepp Et al.
    J Neurosci 2015;35:1052
  18. 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
  19. Soluble epoxide hydrolase inhibitor enhances synaptic neurotransmission and plasticity in mouse prefrontal cortex.
    Authors: Wu Et al.
    J Biomed Sci 2015;22:94
  20. Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus.
    Authors: John Et al.
    Brain Res 2015;1601:15
  21. 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
  22. MARK/Par1 Kinase Is Activated Downstream of NMDA Receptors through a PKA-Dependent Mechanism.
    Authors: Bernard and Zhang
    PLoS One 2015;10:e0124816
  23. Daily isoflurane 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
  24. 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
  25. 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
  26. Imaging intraorganellar Ca2+ at subcellular resolution using CEPIA.
    Authors: Suzuki Et al.
    Nat Commun 2014;5:4153
  27. 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
  28. 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
  29. CaMKII phosphorylation of neuroligin-1 regulates excitatory synapses.
    Authors: Bemben Et al.
    Nat Neurosci 2014;17:56
  30. 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
  31. 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
  32. Synapsin II desynchronizes neurotransmitter release at inhibitory synapses by interacting with presynaptic calcium channels.
    Authors: Medrihan Et al.
    Nat Commun 2013;4:1512
  33. 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
  34. 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
  35. 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
  36. 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
  37. Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity.
    Authors: Korb Et al.
    Nat Neurosci 2013;16:874
  38. Plasticity-related gene 3 promotes neurite shaft protrusion.
    Authors: Velmans Et al.
    BMC Neurosci 2013;14:36
  39. Synaptic and extrasynaptic transmission of kidney-related neurons in the rostral ventrolateral medulla.
    Authors: Gao and Derbenev
    J Neurophysiol 2013;110:2637
  40. Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons.
    Authors: Kaufman Et al.
    J Neurosci 2012;32:3992
  41. 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
  42. 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
  43. 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
  44. Uncoupling the roles of synaptotagmin I during endo- and exocytosis of synaptic vesicles.
    Authors: Yao Et al.
    Nat Neurosci 2012;15:243
  45. Basolateral amygdala inactivation impairs learning-induced long-term potentiation in the cerebellar cortex.
    Authors: Zhu Et al.
    PLoS One 2011;6:e16673
  46. Sleep-deprivation regulates α-2 adrenergic responses of rat hypocretin/orexin neurons.
    Authors: Uschakov Et al.
    PLoS One 2011;6:e16672
  47. 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
  48. 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
  49. SV2 mediates entry of tetanus neurotoxin into central neurons.
    Authors: Yeh Et al.
    PLoS Pathog 2010;6:e1001207
  50. Selected SALM (synaptic adhesion-like molecule) family proteins regulate synapse formation.
    Authors: Mah Et al.
    J Neurosci 2010;30:5559
  51. Estradiol acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism.
    Authors: Smejkalova and Woolley
    J Neurosci 2010;30:16137
  52. Cannabinoids excite circadian clock neurons.
    Authors: Acuna-Goycolea Et al.
    J Neurosci 2010;30:10061
  53. Imaging activity-dependent regulation of neurexin-neuroligin interactions using trans-synaptic enzymatic biotinylation.
    Authors: Thyagarajan and Ting
    Cell 2010;143:456
  54. Characterization of engineered channelrhodopsin variants with improved properties and kinetics.
    Authors: Lin Et al.
    Biophys J 2009;96:1803
  55. 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
  56. Novel repression of Kcc2 transcription by REST-RE-1 controls developmental switch in neuronal chloride.
    Authors: Yeo Et al.
    J Neurosci 2009;29:14652
  57. 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
  58. Histone H2AX-dependent GABA(A) receptor regulation of stem cell proliferation.
    Authors: Andäng Et al.
    Nature 2008;451:460
  59. 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
  60. 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
  61. 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
  62. A nitric oxide signaling pathway controls CREB-mediated gene expression in neurons.
    Authors: Riccio Et al.
    Mol Cell 2006;21:283
  63. Glutamatergic regulation of the p70S6 kinase in primary mouse neurons.
    Authors: Lenz and Avruch
    J Biol Chem 2005;280:38121
  64. Distinct γ2 subunit domains mediate clustering and synaptic function of postsynaptic GABAA receptors and gephyrin.
    Authors: Alldred Et al.
    J Neurosci 2005;25:594
  65. Propofol 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
  66. 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
  67. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci 2004;24:4551
Expand to show all 67 Citations

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