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Submit Review(+)-Bicuculline
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
Purity: ≥99% (HPLC)
Biological Activity for (+)-Bicuculline
(+)-Bicuculline is a classical GABAA antagonist.
Methoiodide Salt, Methobromide Salt and Methochloride Salt also available.
Technical Data for (+)-Bicuculline
| M. Wt | 367.36 |
| Formula | C20H17NO6 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 485-49-4 |
| PubChem ID | 10237 |
| InChI Key | IYGYMKDQCDOMRE-ZWKOTPCHSA-N |
| Smiles | [H][C@](C(C=CC6=C5OCO6)=C5C(O4)=O)4[C@]2([H])C1=CC3=C(OCO3)C=C1CCN2C |
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 (+)-Bicuculline
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.74 | 100 |
Preparing Stock Solutions for (+)-Bicuculline
The following data is based on the product molecular weight 367.36. 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 |
|---|---|---|---|
| 1 mM | 2.72 mL | 13.61 mL | 27.22 mL |
| 5 mM | 0.54 mL | 2.72 mL | 5.44 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.72 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for (+)-Bicuculline
References for (+)-Bicuculline
References are publications that support the biological activity of the product.
Curtis et al (1970) GABA, bicuculline and central inhibition. Nature 226 1222 PMID: 4393081
Olsen et al (1976) Studies on the neuropharmacological activity of bicuculline and related compounds. Brain Res. 102 283 PMID: 1247886
Piredda et al (1985) Intracerebral site of convulsant action of bicuculline. Life Sci. 36 1295 PMID: 3982215
Sieghart et al (1989) Multiplicity of GABAA-benzodiazepine receptors. TiPS 10 407 PMID: 2559519
Merck Index 12 1250
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Keywords: (+)-Bicuculline, (+)-Bicuculline supplier, Potent, GABAA, antagonists, Receptors, 0130, Tocris Bioscience
99 Citations for (+)-Bicuculline
Citations are publications that use Tocris products. Selected citations for (+)-Bicuculline include:
He et al (2020) Nucleus Accumbens Tac1-Expressing Neurons Mediate Stress-Induced Anhedonia-like Behavior in Mice Cell Rep 33 PMID: 33147466
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Zhu et al (2017) Impairments of spatial memory in an Alzheimer's disease model via degeneration of hippocampal cholinergic synapses. Nat Commun 8 1676 PMID: 29162816
Li et al (2017) Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity. Cell 168 86 PMID: 27916275
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Gaffaney et al (2014) Mutations that disrupt Ca2+-binding activity endow Doc2β with novel functional properties during synaptic transmission. Mol Biol Cell 25 481 PMID: 24356452
Velmans et al (2013) Plasticity-related gene 3 promotes neurite shaft protrusion. BMC Neurosci 14 36 PMID: 23506325
Korb et al (2013) Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity. Nat Neurosci 16 874 PMID: 23749147
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Berlinguer-Palmini et al (2013) GPR35 activation reduces Ca2+ transients and contributes to the kynurenic acid-dependent reduction of synaptic activity at CA3-CA1 synapses. PLoS One 8 e82180 PMID: 24312407
Hur and Park (2013) Long-term potentiation of excitatory synaptic strength in spinothalamic tract neurons of the rat spinal cord. Korean J Physiol Pharmacol 17 553 PMID: 24381506
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Bernard and Zhang (2015) MARK/Par1 Kinase Is Activated Downstream of NMDA Receptors through a PKA-Dependent Mechanism. PLoS One 10 e0124816 PMID: 25932647
Curtin and Preuss (2015) Glycine and GABAA receptors mediate tonic and phasic inhibitory processes that contribute to prepulse inhibition in the goldfish startle network. Front Neural Circuits 9 12 PMID: 25852486
Oostland et al (2014) Distinct temporal expression of 5-HT(1A) and 5-HT(2A) receptors on cerebellar granule cells in mice. Cerebellum 13 491 PMID: 24788088
Chen et al (2014) Activation of mGluR2/3 underlies the effects of N-acetylcystein on amygdala-associated autism-like phenotypes in a valproate-induced rat model of autism. Front Behav Neurosci 8 219 PMID: 24987341
Gangadharan et al (2011) Peripheral calcium-permeable AMPA receptors regulate chronic inflammatory pain in mice. J Clin Invest 121 1608 PMID: 21383497
Yue et al (2011) Potentiating action of PropF. at GABAA receptors of retinal bipolar cells. Invest Ophthalmol Vis Sci 52 2497 PMID: 21071744
Zhang et al (2009) Tamoxifen mediated estrogen receptor activation protects against early impairment of hippocampal neuron excitability in an oxygen/glucose deprivation brain slice ischemia model. Brain Res 1247 196 PMID: 18992727
Young and Neher (2009) Synaptotagmin has an essential function in synaptic vesicle positioning for synchronous release in addition to its role as a calcium sensor. Neuron 63 482 PMID: 19709630
Velden et al (2019) Modulation of Functional Connectivity Between DA Neurons of the Rat Ventral Tegmental Area in vitro. Front Integr Neurosci 13 20 PMID: 31293395
Wagner et al (2019) Myosin VI Drives Clathrin-Mediated AMPA Receptor Endocytosis to Facilitate Cerebellar Long-Term Depression. Cell Rep 28 11 PMID: 31269433
Montandon (2017) δ-subunit containing GABAA receptors modulate respiratory networks. Sci Rep 7 18105 PMID: 29273726
Scudder and Patrick (2015) Synaptic structure and function are altered by the neddylation inhibitor MLN4924. Mol Cell Neurosci 65 52 PMID: 25701678
Accardi et al (2015) α6-Containing GABAA Receptors Are the Principal Mediators of Inhibitory Synapse Strengthening by Ins in Cerebellar Granule Cells. J Neurosci 35 9676 PMID: 26134650
Telese et al (2015) LRP8-Reelin-Regulated Neuronal Enhancer Signature Underlying Learning and Memory Formation. Neuron 86 696 PMID: 25892301
Ciani et al (2015) Wnt signalling tunes neurotransmitter release by directly targeting Synaptotagmin-1. Nat Commun 6 8302 PMID: 26400647
Hengen et al (2015) Daily isofl. exposure increases barbiturate insensitivity in medullary respiratory and cortical neurons via expression of η-subunit containing GABA ARs. PLoS One 10 e0119351 PMID: 25748028
Wu et al (2015) Soluble epoxide hydrolase inhibitor enhances synaptic neurotransmission and plasticity in mouse prefrontal cortex. J Biomed Sci 22 94 PMID: 26494028
Morini et al (2015) Subventricular zone neural progenitors reverse TNF-α effects in cortical neurons. Stem Cell Res Ther 6 166 PMID: 26345473
Pappas et al (2015) Forebrain deletion of the dystonia protein torsinA causes dystonic-like movements and loss of striatal cholinergic neurons. Elife 4 e08352 PMID: 26052670
Campbell et al (2015) Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia. Front Cell Neurosci 8 425 PMID: 25565960
Curcio et al (2015) Brain ischemia downregulates the neuroprotective GDNF-Ret signaling by a calpain-dependent mechanism in cultured hippocampal neurons. Cell Death Dis 6 e1645 PMID: 25675305
Huckstepp et al (2015) Role of parafacial nuclei in control of breathing in adult rats. J Neurosci 35 1052 PMID: 25609622
Puranam et al (2015) Disruption of Fgf13 causes synaptic excitatory-inhibitory imbalance and genetic epilepsy and febrile seizures plus. J Neurosci 35 8866 PMID: 26063919
Baquero et al (2015) Developmental changes in synaptic distribution in arcuate nucleus neurons. J Neurosci 35 8558 PMID: 26041922
John et al (2015) Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus. Brain Res 1601 15 PMID: 25553616
Lee et al (2015) N-MthD.-aspartate receptors mediate activity-dependent down-regulation of potassium channel genes during the expression of homeostatic intrinsic plasticity. Mol Brain 8 4 PMID: 25599691
Quintana et al (2015) Acid-sensing ion channel 1a drives AMPA receptor plasticity following ischaemia and acidosis in hippocampal CA1 neurons. J Physiol 593 4373 PMID: 26174503
Zimmermann et al (2015) Co-release of glutamate and GABA from single vesicles in GABAergic neurons exogenously expressing VGLUT3. Front Synaptic Neurosci 7 16 PMID: 26441632
Ding et al (2015) The reinforcing effects of ethanol within the nucleus accumbens shell involve activation of local GABA and serotonin receptors. J Psychopharmacol 29 725 PMID: 25922425
Kangarlu-Haghighi et al (2015) The effect of BLA GABA(A) receptors in anxiolytic-like effect and aversive memory deficit induced by ACPA. EXCLI J 14 613 PMID: 26648818
Robinson et al (2015) Tissue plasminogen activator inhibits NMDA-receptor-mediated increases in calcium levels in cultured hippocampal neurons. Front Cell Neurosci 9 404 PMID: 26500501
Weston et al (2012) Multiple roles for mammalian target of rapamycin signaling in both glutamatergic and GABAergic synaptic transmission. J Neurosci 32 11441 PMID: 22895726
Gil et al (2008) Transient allodynia pain models in mice for early assessment of analgesic activity. Br J Pharmacol 153 769 PMID: 17700719
Zhang et al (2008) Resveratrol attenuates early pyramidal neuron excitability impairment and death in acute rat hippocampal slices caused by oxygen-glucose deprivation. Exp Neurol 212 44 PMID: 18495119
Koeglsperger et al (2013) Impaired glutamate recycling and GluN2B-mediated neuronal calcium overload in mice lacking TGF-β1 in the CNS. Glia 61 985 PMID: 23536313
Deeb et al (2013) Disrupted Cl(-) homeostasis contributes to reductions in the inhibitory efficacy of D.pam during hyperexcited states. Eur J Neurosci 38 2453 PMID: 23627375
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
Gao and Derbenev (2013) Synaptic and extrasynaptic transmission of kidney-related neurons in the rostral ventrolateral medulla. J Neurophysiol 110 2637 PMID: 24027107
Thyagarajan and Ting (2010) Imaging activity-dependent regulation of neurexin-neuroligin interactions using trans-synaptic enzymatic biotinylation. Cell 143 456 PMID: 20933261
Zhao et al (2010) Melatonin potentiates glycine currents through a PLC/PKC signalling pathway in rat retinal ganglion cells. J Physiol 588 2605 PMID: 20519319
Han et al (2010) Reduction in synaptic GABA release contributes to target-selective elevation of PVN neuronal activity in rats with myocardial infarction. Am J Physiol Regul Integr Comp Physiol 299 R129 PMID: 20164200
Imlach et al (2016) Glycinergic dysfunction in a subpopulation of dorsal horn interneurons in a rat model of neuropathic pain Scientific Reports 6 37104 PMID: 27841371
Brown et al (2016) γ-Aminobutyric Acid Type A (GABAA) Receptor Subunits Play a Direct Structural Role in Synaptic Contact Formation via Their N-terminal Extracellular Domains. J Biol Chem 291 13926 PMID: 27129275
Acuña et al (2016) Phosphorylation state-dependent modulation of spinal glycine receptors alleviates inflammatory pain. J Clin Invest 126 2547 PMID: 27270175
Datta et al (2016) Identification of small molecules that improve ATP synthesis defects conferred by Leber's hereditary optic neuropathy mutations. Mitochondrion 30 177 PMID: 27497748
Verstegen et al (2014) Phosphorylation of synapsin I by cyclin-dependent kinase-5 sets the ratio between the resting and recycling pools of synaptic vesicles at hippocampal synapses. J Neurosci 34 7266 PMID: 24849359
Accardi et al (2014) Mitochondrial reactive oxygen species regulate the strength of inhibitory GABA-mediated synaptic transmission. Nat Commun 5 3168 PMID: 24430741
Daftary et al (2012) Essential role of brain-derived neurotrophic factor in the regulation of serotonin transmission in the basolateral amygdala. Neuroscience 224 125 PMID: 22917617
Smejkalova and Woolley (2010) OE acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism. J Neurosci 30 16137 PMID: 21123560
Dinamarca et al (2016) Ring finger protein 10 is a novel synaptonuclear messenger encoding activation of NMDA receptors in hippocampus. Elife 5 PMID: 26977767
Kaufman et al (2012) Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons. J Neurosci 32 3992 PMID: 22442066
Dagostin et al (2012) Increased bursting glutamatergic neurotransmission in an auditory forebrain area of the zebra finch (Taenopygia guttata) induced by auditory stimulation. J Comp Physiol A Neuroethol Sens Neural Behav Phys 198 705 PMID: 22752655
Yao et al (2012) Uncoupling the roles of synaptotagmin I during endo- and exocytosis of synaptic vesicles. Nat Neurosci 15 243 PMID: 22197832
Yamamoto et al (2012) Raf kinase inhibitory protein is required for cerebellar long-term synaptic depression by mediating PKC-dependent MAPK activation. J Neurosci 32 14254 PMID: 23055494
Mou et al (2011) Rapid brain-derived neurotrophic factor-dependent sequestration of amygdala and hippocampal GABA(A) receptors via different tyrosine receptor kinase B-mediated phosphorylation pathways. Neuroscience 176 72 PMID: 21195749
Porcher et al (2011) Positive feedback regulation between γ-aminobutyric acid type A (GABA(A)) receptor signaling and brain-derived neurotrophic factor (BDNF) release in developing neurons. J Biol Chem 286 21667 PMID: 21474450
Acuna-Goycolea et al (2010) Cannabinoids excite circadian clock neurons. J Neurosci 30 10061 PMID: 20668190
Mah et al (2010) Selected SALM (synaptic adhesion-like molecule) family proteins regulate synapse formation. J Neurosci 30 5559 PMID: 20410109
Yeh et al (2010) SV2 mediates entry of tetanus neurotoxin into central neurons. PLoS Pathog 6 e1001207 PMID: 21124874
Zhang et al (2018) Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation. Neuron 98 918 PMID: 29754751
Morel et al (2018) JIP1-Mediated JNK Activation Negatively Regulates Synaptic Plasticity and Spatial Memory. J Neurosci 38 3708 PMID: 29540552
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
Marinangeli et al (2018) AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation. iScience 9 1 PMID: 30368077
Dubal et al (2015) Life extension factor klotho prevents mortality and enhances cognition in hAPP transgenic mice. J Neurosci 35 2358 PMID: 25673831
Medrihan et al (2013) Synapsin II desynchronizes neurotransmitter release at inhibitory synapses by interacting with presynaptic calcium channels. Nat Commun 4 1512 PMID: 23443540
Chen et al (2013) The Munc13 proteins differentially regulate readily releasable pool dynamics and calcium-dependent recovery at a central synapse. J Neurosci 33 8336 PMID: 23658173
Zhu et al (2011) Basolateral amygdala inactivation impairs learning-induced long-term potentiation in the cerebellar cortex. PLoS One 6 e16673 PMID: 21304962
Uschakov et al (2011) Sleep-deprivation regulates α-2 adrenergic responses of rat hypocretin/orexin neurons. PLoS One 6 e16672 PMID: 21347440
Surges et al (2006) Regulated expression of HCN channels and cAMP levels shape the properties of the h current in developing rat hippocampus. Eur J Neurosci 24 94 PMID: 16882011
Brager and Johnston (2007) Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons. J Neurosci 27 13926 PMID: 18094230
Krucker et al (2000) Dynamic actin filaments are required for stable long-term potentiation (LTP) in area CA1 of the hippocampus. Proc Natl Acad Sci U S A 97 6856 PMID: 10823894
Rouaud and Billard (2003) D-cycloserine facilitates synaptic plasticity but impairs glutamatergic neurotransmission in rat hippocampal slices. Br J Pharmacol 140 1051 PMID: 14530208
Ying and Goldstein (2005) PropF. suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels. Mol Pain 1 2 PMID: 15813991
Berghuis et al (2005) Endocannabinoids regulate interneuron migration and morphogenesis by transactivating the TrkB receptor. Proc Natl Acad Sci U S A 102 19115 PMID: 16357196
Alldred et al (2005) Distinct γ2 subunit domains mediate clustering and synaptic function of postsynaptic GABAA receptors and gephyrin. J Neurosci 25 594 PMID: 15659595
Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551 PMID: 15140926
Kuroyanagi et al (2009) Postsynaptic glutamate receptor δ family contributes to presynaptic terminal differentiation and establishment of synaptic transmission. Proc Natl Acad Sci U S A 106 4912 PMID: 19258455
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Use of BIC as a selective GABA-A receptor antagonist.
By
Anonymous on 05/20/2019
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Hippocampus
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.
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