Catalog Number: 1262
Alternate Names: Gabazine
Chemical Name: 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
Biological Activity
Selective, competitive GABAA receptor antagonist. Displaces [3H]-GABA from rat brain membranes with a Ki of 150 nM. Unlike bicuculline, selectively antagonizes GABA-induced Cl- currents with little action on pentobarbitone-induced currents. Also acts as a low affinity glycine receptor antagonist.
Technical Data
  • M.Wt:
    368.23
  • Formula:
    C15H17N3O3.HBr
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    104104-50-9
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.
Background References
  1. The kinetics of inhibition of rat recombinant heterotrimeric α1β glycine receptors by the low affinity antagonist SR-95531.
    Beato et al.
    J.Physiol., 2007;580:171
  2. Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site.
    Heaulme et al.
    Brain Res., 1986;384:224
  3. The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons.
    Uchida et al.
    Eur.J.Pharmacol., 1996;307:89
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SR 95531 hydrobromide include:

114 Citations: Showing 1 - 10
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  1. Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells.
    Authors: Hirono
    Neuropharmacology 2017;118:79
  2. Spontaneous release regulates synaptic scaling in the embryonic spinal network in vivo.
    Authors: Miguel Angel Garcia-Bereguiain Et al.
    The Journal of Neuroscience 2016;6:7268
  3. Differential somatic Ca2+ channel profile in midbrain dopaminergic neurons.
    Authors: Philippart Et al.
    The Journal of Neuroscience 2016;6:7234
  4. A cholinergic basal forebrain feeding circuit modulates appetite suppression
    Authors: Herman Et al.
    Nature 2016;538:253
  5. Electrophysiological Assessment of Serotonin and GABA Neuron Function in the Dorsal Raphe during the Third Trimester Equivalent Developmental Period in Mice(1,2,3).
    Authors: Morton Et al.
    Proc Natl Acad Sci U S A 2016;2
  6. Vasoactive Intestinal Peptide Excites GnRH Neurons in Male and Female Mice.
    Authors: Piet Et al.
    Endocrinology. 2016;157:3621
  7. Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells.
    Authors: Elgueta Et al.
    Microvasc Res 2015;9:6
  8. Cell-type-specific tuning of Cav1.3 Ca(2+)-channels by a C-terminal automodulatory domain.
    Authors: Scharinger Et al.
    Elife 2015;9:309
  9. Stretch induced hyperexcitability of mice callosal pathway.
    Authors: Fan Et al.
    J Neurophysiol 2015;9:292
  10. An excitatory GABA loop operating in vivo.
    Authors: Astorga Et al.
    Front Cell Neurosci 2015;9:275
  11. Interaction of electrically evoked activity with intrinsic dynamics of cultured cortical networks with and without functional fast GABAergic synaptic transmission.
    Authors: Baltz and Voigt
    Front Cell Neurosci 2015;9:272
  12. Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation.
    Authors: Bell Et al.
    J Neurosci 2015;9:115
  13. High salt intake increases blood pressure via BDNF-mediated downregulation of KCC2 and impaired baroreflex inhibition of vasopressin neurons.
    Authors: Choe Et al.
    Front Cell Neurosci 2015;85:549
  14. Chloride transporter KCC2-dependent neuroprotection depends on the N-terminal protein domain.
    Authors: Winkelmann Et al.
    Cell Death Dis 2015;6:e1776
  15. Optical control of NMDA receptors with a diffusible photoswitch.
    Authors: Laprell Et al.
    Front Cell Neurosci 2015;6:8076
  16. RBFOX3/NeuN is Required for Hippocampal Circuit Balance and Function.
    Authors: Wang Et al.
    Sci Rep 2015;5:17383
  17. Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
    Authors: Bocchio Et al.
    Neuropsychopharmacology 2015;40:3015
  18. Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
    Authors: Saunders Et al.
    Elife 2015;4
  19. An excitatory amacrine cell detects object motion and provides feature-selective input to ganglion cells in the mouse retina.
    Authors: Kim Et al.
    Elife 2015;4
  20. CaRuby-Nano: a novel high affinity calcium probe for dual color imaging.
    Authors: Collot Et al.
    Front Cell Neurosci 2015;4
  21. BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells.
    Authors: Hirono Et al.
    Eneuro 2015;35:7082
  22. Prototypic and arkypallidal neurons in the dopamine-intact external globus pallidus.
    Authors: Abdi Et al.
    J Neurosci 2015;35:6667
  23. Muscarinic receptors modulate dendrodendritic inhibitory synapses to sculpt glomerular output.
    Authors: Liu Et al.
    J Negat Results Biomed 2015;35:5680
  24. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
    Authors: Cramer Et al.
    Physiol Rep 2015;35:5664
  25. The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina.
    Authors: Murphy-Baum and Taylor
    Brain 2015;35:13336
  26. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci 2015;35:11252
  27. Afterhyperpolarization (AHP) regulates the frequency and timing of action potentials in the mitral cells of the olfactory bulb: role of olfactory experience.
    Authors: Duménieu Et al.
    PLoS One 2015;3
  28. Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3).
    Authors: Polito Et al.
    J Neurosci 2015;2
  29. Ethanol exposure during the third trimester equivalent does not affect GABAA or AMPA receptor-mediated spontaneous synaptic transmission in rat CA3 pyramidal neurons.
    Authors: Baculis and Valenzuela
    J Neurophysiol 2015;14:19
  30. Tectal microcircuit generating visual selection commands on gaze-controlling neurons.
    Authors: Kardamakis Et al.
    PLoS One 2015;112:E1956
  31. Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice.
    Authors: Wang Et al.
    Eneuro 2015;10:e0139332
  32. The effect of desflurane on neuronal communication at a central synapse.
    Authors: Mapelli Et al.
    Nat Commun 2015;10:e0123534
  33. Spatially reciprocal inhibition of inhibition within a stimulus selection network in the avian midbrain.
    Authors: Goddard Et al.
    PLoS One 2014;9:e85865
  34. Neonatal NMDA receptor blockade disrupts spike timing and glutamatergic synapses in fast spiking interneurons in a NMDA receptor hypofunction model of schizophrenia.
    Authors: Jones Et al.
    Nature 2014;9:e109303
  35. mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
    Authors: Kubota Et al.
    PLoS One 2014;9:e106316
  36. CRISPR/Cas9-mediated gene knock-down in post-mitotic neurons.
    Authors: Straub Et al.
    J Neurophysiol 2014;9:e105584
  37. Inhibitory projections from the ventral nucleus of the trapezoid body to the medial nucleus of the trapezoid body in the mouse.
    Authors: Albrecht Et al.
    Front Neural Circuits 2014;8:83
  38. Regulation of output spike patterns by phasic inhibition in cerebellar granule cells.
    Authors: Nieus Et al.
    Front Cell Neurosci 2014;8:246
  39. Lamina-specific contribution of glutamatergic and GABAergic potentials to hippocampal sharp wave-ripple complexes.
    Authors: Schönberger Et al.
    J Cereb Blood Flow Metab 2014;8:103
  40. Dopamine neurons control striatal cholinergic neurons via regionally heterogeneous dopamine and glutamate signaling.
    Authors: Chuhma Et al.
    PLoS One 2014;81:901
  41. HSF1 transcriptional activity mediates alcohol induction of Vamp2 expression and GABA release.
    Authors: Varodayan and Harrison
    J Neurophysiol 2014;7:89
  42. Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex.
    Authors: Muralidhar Et al.
    Front Neuroanat 2014;7:52
  43. Synapse elimination and learning rules co-regulated by MHC class I H2-Db.
    Authors: Lee Et al.
    Nat Neurosci 2014;509:195
  44. Cross-synaptic synchrony and transmission of signal and noise across the mouse retina.
    Authors: Grimes Et al.
    Elife 2014;3:e03892
  45. Gap junction networks can generate both ripple-like and fast ripple-like oscillations.
    Authors: Simon Et al.
    Eur J Neurosci 2014;39:46
  46. Glycolysis and oxidative phosphorylation in neurons and astrocytes during network activity in hippocampal slices.
    Authors: Ivanov Et al.
    J Cereb Blood Flow Metab 2014;34:397
  47. Three distinct blue-green color pathways in a mammalian retina.
    Authors: Mills Et al.
    J Neurosci 2014;34:1760
  48. Moderate Alcohol Exposure during the Rat Equivalent to the Third Trimester of Human Pregnancy Alters Regulation of GABAA Receptor-Mediated Synaptic Transmission by Dopamine in the Basolateral Amygdala.
    Authors: Diaz Et al.
    J Neurosci 2014;2:46
  49. Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra dopamine neurons.
    Authors: Dragicevic Et al.
    Neuron 2014;137:2287
  50. Depressed GABA and glutamate synaptic signaling by 5-HT1A receptors in the nucleus tractus solitarii and their role in cardiorespiratory function.
    Authors: Ostrowski Et al.
    J Neurosci 2014;111:2493
  51. Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons.
    Authors: Mariqueo Et al.
    Front Pediatr 2014;111:1940
  52. 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
  53. Intersecting circuits generate precisely patterned retinal waves.
    Authors: Akrouh and Kerschensteiner
    Neuron 2013;79:322
  54. Weaker control of the electrical properties of cerebellar granule cells by tonically active GABAA receptors in the Ts65Dn mouse model of Down's syndrome.
    Authors: Szemes Et al.
    Mol Brain 2013;6:33
  55. Properties of the ON bistratified ganglion cell in the rabbit retina.
    Authors: Hoshi Et al.
    J Comp Neurol 2013;521:1497
  56. Autism-related deficits via dysregulated eIF4E-dependent translational control.
    Authors: Gkogkas Et al.
    Proc Natl Acad Sci U S A 2013;493:371
  57. Postnatal loss of P/Q-type channels confined to rhombic-lip-derived neurons alters synaptic transmission at the parallel fiber to purkinje cell synapse and replicates genomic Cacna1a mutation phenotype of ataxia and seizures in mice.
    Authors: Maejima Et al.
    J Neurosci 2013;33:5162
  58. A reorganized GABAergic circuit in a model of epilepsy: evidence from optogenetic labeling and stimulation of somatostatin interneurons.
    Authors: Peng Et al.
    PLoS One 2013;33:14392
  59. Behavioural and functional characterization of Kv10.1 (Eag1) knockout mice.
    Authors: Ufartes Et al.
    Hum Mol Genet 2013;22:2247
  60. GABA(A) receptors implicated in REM sleep control express a benzodiazepine binding site.
    Authors: Nguyen Et al.
    J Biol Chem 2013;1527:131
  61. Synaptic and extrasynaptic transmission of kidney-related neurons in the rostral ventrolateral medulla.
    Authors: Gao and Derbenev
    J Neurosci 2013;110:2637
  62. Olfactory bulb glomerular NMDA receptors mediate olfactory nerve potentiation and odor preference learning in the neonate rat.
    Authors: Lethbridge Et al.
    Mol Pain 2012;7:e35024
  63. Pre and post synaptic NMDA effects targeting Purkinje cells in the mouse cerebellar cortex.
    Authors: Lonchamp Et al.
    PLoS One 2012;7:e30180
  64. Cerebellar globular cells receive monoaminergic excitation and monosynaptic inhibition from Purkinje cells.
    Authors: Hirono Et al.
    PLoS One 2012;7:e29663
  65. Opposing Effects of Intrinsic Conductance and Correlated Synaptic Input on V-Fluctuations during Network Activity.
    Authors: Kolind Et al.
    Front Comput Neurosci 2012;6:40
  66. Brain-derived neurotrophic factor activation of CaM-kinase kinase via transient receptor potential canonical channels induces the translation and synaptic incorporation of GluA1-containing calcium-permeable AMPA receptors.
    Authors: Fortin Et al.
    J Neurosci 2012;32:8127
  67. Optimization of a GCaMP calcium indicator for neural activity imaging.
    Authors: Akerboom Et al.
    J Neurosci 2012;32:13819
  68. Intrinsic modulators of auditory thalamocortical transmission.
    Authors: Lee and Sherman
    Hear Res 2012;287:43
  69. ZD7288 enhances long-term depression at early postnatal medial perforant path-granule cell synapses.
    Authors: Guli Et al.
    Neural Plast 2012;2012:237913
  70. Focal adhesion kinase regulates actin nucleation and neuronal filopodia formation during axonal growth.
    Authors: Chacón Et al.
    Brain Res 2012;139:3200
  71. 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
    Authors: Austgen Et al.
    Cereb Cortex 2012;108:2292
  72. Age-dependent effect of hearing loss on cortical inhibitory synapse function.
    Authors: Takesian Et al.
    J Neurophysiol 2012;107:937
  73. Synaptic responses evoked by tactile stimuli in Purkinje cells in mouse cerebellar cortex Crus II in vivo.
    Authors: Chu Et al.
    PLoS One 2011;6:e22752
  74. Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1.
    Authors: Zschenderlein Et al.
    PLoS One 2011;6:e16116
  75. GABAergic signalling in a neurogenic niche of the turtle spinal cord.
    Authors: Reali Et al.
    J Physiol 2011;589:5633
  76. Development of asymmetric inhibition underlying direction selectivity in the retina.
    Authors: Wei Et al.
    J Neurophysiol 2011;469:402
  77. Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro.
    Authors: Randall Et al.
    Eur J Neurosci 2011;33:914
  78. SK2 channels are neuroprotective for ischemia-induced neuronal cell death.
    Authors: Allen Et al.
    J Neurosci 2011;31:2302
  79. A diversity of synaptic filters are created by temporal summation of excitation and inhibition.
    Authors: George Et al.
    J Neurosci 2011;31:14721
  80. NMDA receptor signaling in oligodendrocyte progenitors is not required for oligodendrogenesis and myelination.
    Authors: Biase Et al.
    J Neurophysiol 2011;31:12650
  81. Rapid developmental maturation of neocortical FS cell intrinsic excitability.
    Authors: Goldberg Et al.
    Front Cell Neurosci 2011;21:666
  82. The SK2-long isoform directs synaptic localization and function of SK2-containing channels.
    Authors: Allen Et al.
    Nat Neurosci 2011;14:744
  83. Hydrogen sulfide augments synaptic neurotransmission in the nucleus of the solitary tract.
    Authors: Austgen Et al.
    J Neurophysiol 2011;106:1822
  84. A portable laser photostimulation and imaging microscope.
    Authors: Nikolenko Et al.
    J Neural Eng 2010;7:45001
  85. Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei.
    Authors: Person and Raman
    Neuron 2010;66:550
  86. High-Pass Filtering and Dynamic Gain Regulation Enhance Vertical Bursts Transmission along the Mossy Fiber Pathway of Cerebellum.
    Authors: Mapelli Et al.
    Nature 2010;4:14
  87. Excitability and synaptic communication within the oligodendrocyte lineage.
    Authors: Biase Et al.
    J Neurosci 2010;30:3600
  88. Orientation selectivity in rabbit retinal ganglion cells is mediated by presynaptic inhibition.
    Authors: Venkataramani and Taylor
    J Neurosci 2010;30:15664
  89. Control of CA3 output by feedforward inhibition despite developmental changes in the excitation-inhibition balance.
    Authors: Torborg Et al.
    J Neurosci 2010;30:15628
  90. Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice.
    Authors: Tani Et al.
    J Neurosci 2010;30:1288
  91. Substitution of 5-HT1A receptor signaling by a light-activated G protein-coupled receptor.
    Authors: Oh Et al.
    Front Neural Circuits 2010;285:30825
  92. Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses.
    Authors: Kim and Alger
    Nat Neurosci 2010;13:592
  93. Glutamate co-release at GABA/glycinergic synapses is crucial for the refinement of an inhibitory map.
    Authors: Noh Et al.
    PLoS One 2010;13:232
  94. Synaptic network activity induces neuronal differentiation of adult hippocampal precursor cells through BDNF signaling.
    Authors: Babu Et al.
    Front Neurosci 2009;3:49
  95. Synaptic circuit abnormalities of motor-frontal layer 2/3 pyramidal neurons in an RNA interference model of methyl-CpG-binding protein 2 deficiency.
    Authors: Wood Et al.
    Chem Senses 2009;29:12440
  96. Propofol inhibits pressure-stimulated macrophage phagocytosis via the GABAA receptor and dysregulation of p130cas phosphorylation.
    Authors: Shiratsuchi Et al.
    Am J Physiol Cell Physiol 2009;296:C1400
  97. Dopamine neuron glutamate cotransmission: frequency-dependent modulation in the mesoventromedial projection.
    Authors: Chuhma Et al.
    Neuroscience 2009;164:1068
  98. Differential endocannabinoid regulation of baroreflex-evoked sympathoinhibition in normotensive versus hypertensive rats.
    Authors: Brozoski Et al.
    Auton Neurosci 2009;150:82
  99. Activity-dependent modulation of glutamatergic signaling in the developing rat dorsal horn by early tissue injury.
    Authors: Li Et al.
    Cereb Cortex 2009;102:2208
  100. Co-transmission of dopamine and GABA in periglomerular cells.
    Authors: Maher and Westbrook
    J Neurophysiol 2008;99:1559
  101. Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys.
    Authors: Darbin and Wichmann
    Front Cell Neurosci 2008;99:1294
  102. Synapse-specific adaptations to inactivity in hippocampal circuits achieve homeostatic gain control while dampening network reverberation.
    Authors: Kim and Tsien
    Neuron 2008;58:925
  103. Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex.
    Authors: Kotak Et al.
    Cereb Cortex 2008;18:2098
  104. Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
    Authors: Shin Et al.
    J Neurosci 2008;105:746
  105. Selective, state-dependent activation of somatostatin-expressing inhibitory interneurons in mouse neocortex.
    Authors: Fanselow Et al.
    J Neurophysiol 2008;100:2640
  106. Long-term modifications in the strength of excitatory associative inputs in the piriform cortex.
    Authors: Young and Sun
    Neuron 2007;32:783
  107. Differential effects of endocannabinoids on glutamatergic and GABAergic inputs to layer 5 pyramidal neurons.
    Authors: Fortin and Levine
    Development 2007;17:163
  108. Vesicular release of glutamate from unmyelinated axons in white matter.
    Authors: Ziskin Et al.
    Front Integr Neurosci 2007;10:321
  109. Regulation of thalamocortical patterning and synaptic maturation by NeuroD2.
    Authors: Ince-Dunn Et al.
    Neuron 2006;49:683
  110. Altered balance of glutamatergic/GABAergic synaptic input and associated changes in dendrite morphology after BDNF expression in BDNF-deficient hippocampal neurons.
    Authors: Singh Et al.
    Nature 2006;26:7189
  111. Inhibitory sharpening of receptive fields contributes to whisker map plasticity in rat somatosensory cortex.
    Authors: Foeller Et al.
    J Neurophysiol 2005;94:4387
  112. Propofol suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels.
    Authors: Ying and Goldstein
    J Neurosci 2005;1:2
  113. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci 2004;24:4551
  114. Localization and function of ATP and GABAA receptors expressed by nociceptors and other postnatal sensory neurons in rat.
    Authors: Labrakakis Et al.
    J Physiol 2003;549:131
Expand to show all 114 Citations

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