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:
  • Formula:
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
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

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

Showing Results 1 - 10 of 112

  1. Spontaneous release regulates synaptic scaling in the embryonic spinal network�in vivo.
    Authors: Miguel Angel Garcia-Bereguiain Et al.
    The Journal of Neuroscience
  2. Differential somatic Ca2+�channel profile in midbrain dopaminergic neurons.
    Authors: Philippart Et al.
    The Journal of Neuroscience
  3. 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
  4. Vasoactive Intestinal Peptide Excites GnRH Neurons in Male and Female Mice.
    Authors: Piet Et al.
  5. Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells.
    Authors: Elgueta Et al.
    Microvasc Res
  6. Cell-type-specific tuning of Cav1.3 Ca(2+)-channels by a C-terminal automodulatory domain.
    Authors: Scharinger Et al.
  7. Stretch induced hyperexcitability of mice callosal pathway.
    Authors: Fan Et al.
    J Neurophysiol
  8. An excitatory GABA loop operating in vivo.
    Authors: Astorga Et al.
    Front Cell Neurosci
  9. 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
  10. Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation.
    Authors: Bell Et al.
    J Neurosci
  11. 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
  12. Chloride transporter KCC2-dependent neuroprotection depends on the N-terminal protein domain.
    Authors: Winkelmann Et al.
    Cell Death Dis
  13. Optical control of NMDA receptors with a diffusible photoswitch.
    Authors: Laprell Et al.
    Front Cell Neurosci
  14. RBFOX3/NeuN is Required for Hippocampal Circuit Balance and Function.
    Authors: Wang Et al.
    Sci Rep
  15. Corelease of acetylcholine and GABA from cholinergic forebrain neurons.
    Authors: Saunders Et al.
  16. An excitatory amacrine cell detects object motion and provides feature-selective input to ganglion cells in the mouse retina.
    Authors: Kim Et al.
  17. CaRuby-Nano: a novel high affinity calcium probe for dual color imaging.
    Authors: Collot Et al.
    Front Cell Neurosci
  18. Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala.
    Authors: Bocchio Et al.
  19. 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
  20. BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells.
    Authors: Hirono Et al.
  21. Prototypic and arkypallidal neurons in the dopamine-intact external globus pallidus.
    Authors: Abdi Et al.
    J Neurosci
  22. Muscarinic receptors modulate dendrodendritic inhibitory synapses to sculpt glomerular output.
    Authors: Liu Et al.
    J Negat Results Biomed
  23. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
    Authors: Cramer Et al.
    Physiol Rep
  24. The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina.
    Authors: Murphy-Baum and Taylor
  25. Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus.
    Authors: Tabatadze Et al.
    J Neurosci
  26. Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3).
    Authors: Polito Et al.
    J Neurosci
  27. 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
  28. Tectal microcircuit generating visual selection commands on gaze-controlling neurons.
    Authors: Kardamakis Et al.
    PLoS One
  29. Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice.
    Authors: Wang Et al.
  30. The effect of desflurane on neuronal communication at a central synapse.
    Authors: Mapelli Et al.
    Nat Commun
  31. Spatially reciprocal inhibition of inhibition within a stimulus selection network in the avian midbrain.
    Authors: Goddard Et al.
    PLoS One
  32. 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.
  33. 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
  34. CRISPR/Cas9-mediated gene knock-down in post-mitotic neurons.
    Authors: Straub Et al.
    J Neurophysiol
  35. 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
  36. Regulation of output spike patterns by phasic inhibition in cerebellar granule cells.
    Authors: Nieus Et al.
    Front Cell Neurosci
  37. Lamina-specific contribution of glutamatergic and GABAergic potentials to hippocampal sharp wave-ripple complexes.
    Authors: Schönberger Et al.
    J Cereb Blood Flow Metab
  38. Dopamine neurons control striatal cholinergic neurons via regionally heterogeneous dopamine and glutamate signaling.
    Authors: Chuhma Et al.
    PLoS One
  39. HSF1 transcriptional activity mediates alcohol induction of Vamp2 expression and GABA release.
    Authors: Varodayan and Harrison
    J Neurophysiol
  40. Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex.
    Authors: Muralidhar Et al.
    Front Neuroanat
  41. Synapse elimination and learning rules co-regulated by MHC class I H2-Db.
    Authors: Lee Et al.
    Nat Neurosci
  42. Cross-synaptic synchrony and transmission of signal and noise across the mouse retina.
    Authors: Grimes Et al.
  43. Gap junction networks can generate both ripple-like and fast ripple-like oscillations.
    Authors: Simon Et al.
    Eur J Neurosci
  44. Glycolysis and oxidative phosphorylation in neurons and astrocytes during network activity in hippocampal slices.
    Authors: Ivanov Et al.
    J Cereb Blood Flow Metab
  45. Three distinct blue-green color pathways in a mammalian retina.
    Authors: Mills Et al.
    J Neurosci
  46. 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
  47. Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra dopamine neurons.
    Authors: Dragicevic Et al.
  48. 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
  49. Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons.
    Authors: Mariqueo Et al.
    Front Pediatr
  50. 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
  51. Intersecting circuits generate precisely patterned retinal waves.
    Authors: Akrouh and Kerschensteiner
  52. 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
  53. Properties of the ON bistratified ganglion cell in the rabbit retina.
    Authors: Hoshi Et al.
    J Comp Neurol
  54. Autism-related deficits via dysregulated eIF4E-dependent translational control.
    Authors: Gkogkas Et al.
    Proc Natl Acad Sci U S A
  55. 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
  56. A reorganized GABAergic circuit in a model of epilepsy: evidence from optogenetic labeling and stimulation of somatostatin interneurons.
    Authors: Peng Et al.
    PLoS One
  57. Behavioural and functional characterization of Kv10.1 (Eag1) knockout mice.
    Authors: Ufartes Et al.
    Hum Mol Genet
  58. GABA(A) receptors implicated in REM sleep control express a benzodiazepine binding site.
    Authors: Nguyen Et al.
    J Biol Chem
  59. Synaptic and extrasynaptic transmission of kidney-related neurons in the rostral ventrolateral medulla.
    Authors: Gao and Derbenev
    J Neurosci
  60. Olfactory bulb glomerular NMDA receptors mediate olfactory nerve potentiation and odor preference learning in the neonate rat.
    Authors: Lethbridge Et al.
    Mol Pain
  61. Pre and post synaptic NMDA effects targeting Purkinje cells in the mouse cerebellar cortex.
    Authors: Lonchamp Et al.
    PLoS One
  62. Cerebellar globular cells receive monoaminergic excitation and monosynaptic inhibition from Purkinje cells.
    Authors: Hirono Et al.
    PLoS One
  63. Opposing Effects of Intrinsic Conductance and Correlated Synaptic Input on V-Fluctuations during Network Activity.
    Authors: Kolind Et al.
    Front Comput Neurosci
  64. 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
  65. Optimization of a GCaMP calcium indicator for neural activity imaging.
    Authors: Akerboom Et al.
    J Neurosci
  66. Intrinsic modulators of auditory thalamocortical transmission.
    Authors: Lee and Sherman
    Hear Res
  67. ZD7288 enhances long-term depression at early postnatal medial perforant path-granule cell synapses.
    Authors: Guli Et al.
    Neural Plast
  68. Focal adhesion kinase regulates actin nucleation and neuronal filopodia formation during axonal growth.
    Authors: Chacón Et al.
    Brain Res
  69. 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii.
    Authors: Austgen Et al.
    Cereb Cortex
  70. Age-dependent effect of hearing loss on cortical inhibitory synapse function.
    Authors: Takesian Et al.
    J Neurophysiol
  71. Synaptic responses evoked by tactile stimuli in Purkinje cells in mouse cerebellar cortex Crus II in vivo.
    Authors: Chu Et al.
    PLoS One
  72. Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1.
    Authors: Zschenderlein Et al.
    PLoS One
  73. GABAergic signalling in a neurogenic niche of the turtle spinal cord.
    Authors: Reali Et al.
    J Physiol
  74. Development of asymmetric inhibition underlying direction selectivity in the retina.
    Authors: Wei Et al.
    J Neurophysiol
  75. Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro.
    Authors: Randall Et al.
    Eur J Neurosci
  76. SK2 channels are neuroprotective for ischemia-induced neuronal cell death.
    Authors: Allen Et al.
    J Neurosci
  77. A diversity of synaptic filters are created by temporal summation of excitation and inhibition.
    Authors: George Et al.
    J Neurosci
  78. NMDA receptor signaling in oligodendrocyte progenitors is not required for oligodendrogenesis and myelination.
    Authors: Biase Et al.
    J Neurophysiol
  79. Rapid developmental maturation of neocortical FS cell intrinsic excitability.
    Authors: Goldberg Et al.
    Front Cell Neurosci
  80. The SK2-long isoform directs synaptic localization and function of SK2-containing channels.
    Authors: Allen Et al.
    Nat Neurosci
  81. Hydrogen sulfide augments synaptic neurotransmission in the nucleus of the solitary tract.
    Authors: Austgen Et al.
    J Neurophysiol
  82. A portable laser photostimulation and imaging microscope.
    Authors: Nikolenko Et al.
    J Neural Eng
  83. Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei.
    Authors: Person and Raman
  84. High-Pass Filtering and Dynamic Gain Regulation Enhance Vertical Bursts Transmission along the Mossy Fiber Pathway of Cerebellum.
    Authors: Mapelli Et al.
  85. Excitability and synaptic communication within the oligodendrocyte lineage.
    Authors: Biase Et al.
    J Neurosci
  86. Orientation selectivity in rabbit retinal ganglion cells is mediated by presynaptic inhibition.
    Authors: Venkataramani and Taylor
    J Neurosci
  87. Control of CA3 output by feedforward inhibition despite developmental changes in the excitation-inhibition balance.
    Authors: Torborg Et al.
    J Neurosci
  88. Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice.
    Authors: Tani Et al.
    J Neurosci
  89. Substitution of 5-HT1A receptor signaling by a light-activated G protein-coupled receptor.
    Authors: Oh Et al.
    Front Neural Circuits
  90. Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses.
    Authors: Kim and Alger
    Nat Neurosci
  91. Glutamate co-release at GABA/glycinergic synapses is crucial for the refinement of an inhibitory map.
    Authors: Noh Et al.
    PLoS One
  92. Synaptic network activity induces neuronal differentiation of adult hippocampal precursor cells through BDNF signaling.
    Authors: Babu Et al.
    Front Neurosci
  93. 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
  94. Propofol inhibits pressure-stimulated macrophage phagocytosis via the GABAA receptor and dysregulation of p130cas phosphorylation.
    Authors: Shiratsuchi Et al.
    Am J Physiol Cell Physiol
  95. Dopamine neuron glutamate cotransmission: frequency-dependent modulation in the mesoventromedial projection.
    Authors: Chuhma Et al.
  96. Differential endocannabinoid regulation of baroreflex-evoked sympathoinhibition in normotensive versus hypertensive rats.
    Authors: Brozoski Et al.
    Auton Neurosci
  97. Activity-dependent modulation of glutamatergic signaling in the developing rat dorsal horn by early tissue injury.
    Authors: Li Et al.
    Cereb Cortex
  98. Co-transmission of dopamine and GABA in periglomerular cells.
    Authors: Maher and Westbrook
    J Neurophysiol
  99. Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys.
    Authors: Darbin and Wichmann
    Front Cell Neurosci
  100. Synapse-specific adaptations to inactivity in hippocampal circuits achieve homeostatic gain control while dampening network reverberation.
    Authors: Kim and Tsien
  101. Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex.
    Authors: Kotak Et al.
    Cereb Cortex
  102. Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells.
    Authors: Shin Et al.
    J Neurosci
  103. Selective, state-dependent activation of somatostatin-expressing inhibitory interneurons in mouse neocortex.
    Authors: Fanselow Et al.
    J Neurophysiol
  104. Long-term modifications in the strength of excitatory associative inputs in the piriform cortex.
    Authors: Young and Sun
  105. Differential effects of endocannabinoids on glutamatergic and GABAergic inputs to layer 5 pyramidal neurons.
    Authors: Fortin and Levine
  106. Vesicular release of glutamate from unmyelinated axons in white matter.
    Authors: Ziskin Et al.
    Front Integr Neurosci
  107. Regulation of thalamocortical patterning and synaptic maturation by NeuroD2.
    Authors: Ince-Dunn Et al.
  108. 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.
  109. Inhibitory sharpening of receptive fields contributes to whisker map plasticity in rat somatosensory cortex.
    Authors: Foeller Et al.
    J Neurophysiol
  110. Propofol suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels.
    Authors: Ying and Goldstein
    J Neurosci
  111. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci
  112. Localization and function of ATP and GABAA receptors expressed by nociceptors and other postnatal sensory neurons in rat.
    Authors: Labrakakis Et al.
    J Physiol
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