SR 95531 hydrobromide

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Cat.No. 1262 - SR 95531 hydrobromide | C15H17N3O3.HBr | CAS No. 104104-50-9
Description: Selective, competitive GABAA receptor antagonist
Alternative Names: Gabazine
Chemical Name: 6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridazinebutanoic acid hydrobromide
Purity: ≥98% (HPLC)
Datasheet
Citations (114)
Literature

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.

Compound Libraries

SR 95531 hydrobromide is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 368.23
Formula C15H17N3O3.HBr
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 104104-50-9
PubChem ID 11056106
InChI Key VVDXNJRUNJMYOZ-DHXVBOOMSA-N
Smiles Br.COC1=CC=C(C=C1)C1=NN(CCCC(O)=O)C(=N)C=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.82 100
ethanol 7.36 20
water 9.21 25
phosphate buffered saline 1.84 5

Preparing Stock Solutions

The following data is based on the product molecular weight 368.23. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.72 mL 13.58 mL 27.16 mL
5 mM 0.54 mL 2.72 mL 5.43 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Beato et al (2007) The kinetics of inhibition of rat recombinant heterotrimeric α1β glycine receptors by the low affinity antagonist SR-95531. J.Physiol. 580 171 PMID: 17218350

Heaulme et al (1986) Biochemical characterization of the interaction of three pyridazinyl-GABA derivatives with the GABAA receptor site. Brain Res. 384 224 PMID: 3022866

Uchida et al (1996) The differential antagonism by bicuculline and SR95531 of pentobarbitone-induced currents in cultured hippocampal neurons. Eur.J.Pharmacol. 307 89 PMID: 8831109


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Keywords: Selective competitive GABAA receptor antagonists Receptors SR95531 hydrobromide Gabazine GABAA Receptors

114 Citations for SR 95531 hydrobromide

Citations are publications that use Tocris products. Selected citations for SR 95531 hydrobromide include:

Hirono (2017) Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells. Neuropharmacology 118 79 PMID: 28300552

Miguel Angel Garcia-Bereguiain et al (2016) Spontaneous release regulates synaptic scaling in the embryonic spinal network in vivo. The Journal of Neuroscience 6 7268 PMID: 27383600

Philippart et al (2016) Differential somatic Ca2+ channel profile in midbrain dopaminergic neurons. The Journal of Neuroscience 6 7234 PMID: 27383597

Morton et al (2016) Electrophysiological Assessment of Serotonin and GABA Neuron Function in the Dorsal Raphe during the Third Trimester Equivalent Developmental Period in Mice(1,2,3). Proc Natl Acad Sci U S A 2 PMID: 26730407

Herman et al (2016) A cholinergic basal forebrain feeding circuit modulates appetite suppression Nature 538 253 PMID: 27698417

Piet et al (2016) Vasoactive Intestinal Peptide Excites GnRH Neurons in Male and Female Mice. Endocrinology. 157 3621 PMID: 27501185

Wang et al (2015) RBFOX3/NeuN is Required for Hippocampal Circuit Balance and Function. Sci Rep 5 17383 PMID: 26619789

Winkelmann et al (2015) Chloride transporter KCC2-dependent neuroprotection depends on the N-terminal protein domain. Cell Death Dis 6 e1776 PMID: 26043076

Astorga et al (2015) An excitatory GABA loop operating in vivo. Front Cell Neurosci 9 275 PMID: 26236197

Kim et al (2015) An excitatory amacrine cell detects object motion and provides feature-selective input to ganglion cells in the mouse retina. Elife 4 PMID: 25988808

Baltz and Voigt (2015) Interaction of electrically evoked activity with intrinsic dynamics of cultured cortical networks with and without functional fast GABAergic synaptic transmission. Front Cell Neurosci 9 272 PMID: 26236196

Tabatadze et al (2015) Sex Differences in Molecular Signaling at Inhibitory Synapses in the Hippocampus. J Neurosci 35 11252 PMID: 26269634

Liu et al (2015) Muscarinic receptors modulate dendrodendritic inhibitory synapses to sculpt glomerular output. J Negat Results Biomed 35 5680 PMID: 25855181

Elgueta et al (2015) Acetylcholine induces GABA release onto rod bipolar cells through heteromeric nicotinic receptors expressed in A17 amacrine cells. Microvasc Res 9 6 PMID: 25709566

Kardamakis et al (2015) Tectal microcircuit generating visual selection commands on gaze-controlling neurons. PLoS One 112 E1956 PMID: 25825743

Mapelli et al (2015) The effect of desflurane on neuronal communication at a central synapse. Nat Commun 10 e0123534 PMID: 25849222

Laprell et al (2015) Optical control of NMDA receptors with a diffusible photoswitch. Front Cell Neurosci 6 8076 PMID: 26311290

Fan et al (2015) Stretch induced hyperexcitability of mice callosal pathway. J Neurophysiol 9 292 PMID: 26300729

Hirono et al (2015) BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells. Eneuro 35 7082 PMID: 25948259

Polito et al (2015) Selective Effects of PDE10A Inhibitors on Striatopallidal Neurons Require Phosphatase Inhibition by DARPP-32(1,2,3). J Neurosci 2 PMID: 26465004

Abdi et al (2015) Prototypic and arkypallidal neurons in the dopamine-intact external globus pallidus. J Neurosci 35 6667 PMID: 25926446

Cramer et al (2015) Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse. Physiol Rep 35 5664 PMID: 25855180

Duménieu et al (2015) Afterhyperpolarization (AHP) regulates the frequency and timing of action potentials in the mitral cells of the olfactory bulb: role of olfactory experience. PLoS One 3 PMID: 26019289

Wang et al (2015) Apamin Boosting of Synaptic Potentials in CaV2.3 R-Type Ca2+ Channel Null Mice. Eneuro 10 e0139332 PMID: 26418566

Choe et al (2015) High salt intake increases blood pressure via BDNF-mediated downregulation of KCC2 and impaired baroreflex inhibition of vasopressin neurons. Front Cell Neurosci 85 549 PMID: 25619659

Scharinger et al (2015) Cell-type-specific tuning of Cav1.3 Ca(2+)-channels by a C-terminal automodulatory domain. Elife 9 309 PMID: 26379493

Saunders et al (2015) Corelease of acetylcholine and GABA from cholinergic forebrain neurons. Elife 4 PMID: 25723967

Collot et al (2015) CaRuby-Nano: a novel high affinity calcium probe for dual color imaging. Front Cell Neurosci 4 PMID: 25824291

Bell et al (2015) Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation. J Neurosci 9 115 PMID: 25918499

Bocchio et al (2015) Increased serotonin transporter expression reduces fear and recruitment of parvalbumin interneurons of the amygdala. Neuropsychopharmacology 40 3015 PMID: 26052039

Murphy-Baum and Taylor (2015) The Synaptic and Morphological Basis of Orientation Selectivity in a Polyaxonal Amacrine Cell of the Rabbit Retina. Brain 35 13336 PMID: 26424882

Baculis and Valenzuela (2015) Ethanol exposure during the third trimester equivalent does not affect GABAA or AMPA receptor-mediated spontaneous synaptic transmission in rat CA3 pyramidal neurons. J Neurophysiol 14 19 PMID: 26627643

Ivanov et al (2014) Glycolysis and oxidative phosphorylation in neurons and astrocytes during network activity in hippocampal slices. J Cereb Blood Flow Metab 34 397 PMID: 24326389

Albrecht et al (2014) Inhibitory projections from the ventral nucleus of the trapezoid body to the medial nucleus of the trapezoid body in the mouse. Front Neural Circuits 8 83 PMID: 25120436

Nieus et al (2014) Regulation of output spike patterns by phasic inhibition in cerebellar granule cells. Front Cell Neurosci 8 246 PMID: 25202237

Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316 PMID: 25181481

Grimes et al (2014) Cross-synaptic synchrony and transmission of signal and noise across the mouse retina. Elife 3 e03892 PMID: 25180102

Mills et al (2014) Three distinct blue-green color pathways in a mammalian retina. J Neurosci 34 1760 PMID: 24478358

Simon et al (2014) Gap junction networks can generate both ripple-like and fast ripple-like oscillations. Eur J Neurosci 39 46 PMID: 24118191

Goddard et al (2014) Spatially reciprocal inhibition of inhibition within a stimulus selection network in the avian midbrain. PLoS One 9 e85865 PMID: 24465755

Muralidhar et al (2014) Synaptic and cellular organization of layer 1 of the developing rat somatosensory cortex. Front Neuroanat 7 52 PMID: 24474905

Straub et al (2014) CRISPR/Cas9-mediated gene knock-down in post-mitotic neurons. J Neurophysiol 9 e105584 PMID: 25140704

Mariqueo et al (2014) Effects of ethanol on glycinergic synaptic currents in mouse spinal cord neurons. Front Pediatr 111 1940 PMID: 24572089

Diaz et al (2014) 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. J Neurosci 2 46 PMID: 24904907

Chuhma et al (2014) Dopamine neurons control striatal cholinergic neurons via regionally heterogeneous dopamine and glutamate signaling. PLoS One 81 901 PMID: 24559678

Dragicevic et al (2014) Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra dopamine neurons. Neuron 137 2287 PMID: 24934288

Lee et al (2014) Synapse elimination and learning rules co-regulated by MHC class I H2-Db. Nat Neurosci 509 195 PMID: 24695230

Jones et al (2014) Neonatal NMDA receptor blockade disrupts spike timing and glutamatergic synapses in fast spiking interneurons in a NMDA receptor hypofunction model of schizophrenia. Nature 9 e109303 PMID: 25290690

Ostrowski et al (2014) Depressed GABA and glutamate synaptic signaling by 5-HT1A receptors in the nucleus tractus solitarii and their role in cardiorespiratory function. J Neurosci 111 2493 PMID: 24671532

Schönberger et al (2014) Lamina-specific contribution of glutamatergic and GABAergic potentials to hippocampal sharp wave-ripple complexes. J Cereb Blood Flow Metab 8 103 PMID: 25202239

Varodayan and Harrison (2014) HSF1 transcriptional activity mediates alcohol induction of Vamp2 expression and GABA release. J Neurophysiol 7 89 PMID: 24376402

Szemes et al (2013) Weaker control of the electrical properties of cerebellar granule cells by tonically active GABAA receptors in the Ts65Dn mouse model of Down's syndrome. Mol Brain 6 33 PMID: 23870245

Ufartes et al (2013) Behavioural and functional characterization of Kv10.1 (Eag1) knockout mice. Hum Mol Genet 22 2247 PMID: 23424202

Hoshi et al (2013) Properties of the ON bistratified ganglion cell in the rabbit retina. J Comp Neurol 521 1497 PMID: 23047654

Akrouh and Kerschensteiner (2013) Intersecting circuits generate precisely patterned retinal waves. Neuron 79 322 PMID: 23830830

Maejima et al (2013) 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. J Neurosci 33 5162 PMID: 23516282

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

Nguyen et al (2013) GABA(A) receptors implicated in REM sleep control express a benzodiazepine binding site. J Biol Chem 1527 131 PMID: 23835499

Gkogkas et al (2013) Autism-related deficits via dysregulated eIF4E-dependent translational control. Proc Natl Acad Sci U S A 493 371 PMID: 23172145

Peng et al (2013) A reorganized GABAergic circuit in a model of epilepsy: evidence from optogenetic labeling and stimulation of somatostatin interneurons. PLoS One 33 14392 PMID: 24005292

Gao and Derbenev (2013) Synaptic and extrasynaptic transmission of kidney-related neurons in the rostral ventrolateral medulla. J Neurosci 110 2637 PMID: 24027107

Guli et al (2012) ZD7288 enhances long-term depression at early postnatal medial perforant path-granule cell synapses. Neural Plast 2012 237913 PMID: 22792490

Takesian et al (2012) Age-dependent effect of hearing loss on cortical inhibitory synapse function. J Neurophysiol 107 937 PMID: 22090457

Akerboom et al (2012) Optimization of a GCaMP calcium indicator for neural activity imaging. J Neurosci 32 13819 PMID: 23035093

Kolind et al (2012) Opposing Effects of Intrinsic Conductance and Correlated Synaptic Input on V-Fluctuations during Network Activity. Front Comput Neurosci 6 40 PMID: 22783184

Fortin et al (2012) 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. J Neurosci 32 8127 PMID: 22699894

Hirono et al (2012) Cerebellar globular cells receive monoaminergic excitation and monosynaptic inhibition from Purkinje cells. PLoS One 7 e29663 PMID: 22235322

Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616

Lonchamp et al (2012) Pre and post synaptic NMDA effects targeting Purkinje cells in the mouse cerebellar cortex. PLoS One 7 e30180 PMID: 22276158

Lethbridge et al (2012) Olfactory bulb glomerular NMDA receptors mediate olfactory nerve potentiation and odor preference learning in the neonate rat. Mol Pain 7 e35024 PMID: 22496886

Chacón et al (2012) Focal adhesion kinase regulates actin nucleation and neuronal filopodia formation during axonal growth. Brain Res 139 3200 PMID: 22872087

Austgen et al (2012) 5-hydroxytryptamine 2C receptors tonically augment synaptic currents in the nucleus tractus solitarii. Cereb Cortex 108 2292 PMID: 22855775

Reali et al (2011) GABAergic signalling in a neurogenic niche of the turtle spinal cord. J Physiol 589 5633 PMID: 21911613

Allen et al (2011) The SK2-long isoform directs synaptic localization and function of SK2-containing channels. Nat Neurosci 14 744 PMID: 21602822

Chu et al (2011) Synaptic responses evoked by tactile stimuli in Purkinje cells in mouse cerebellar cortex Crus II in vivo. PLoS One 6 e22752 PMID: 21818384

Randall et al (2011) Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro. Eur J Neurosci 33 914 PMID: 21255131

George et al (2011) A diversity of synaptic filters are created by temporal summation of excitation and inhibition. J Neurosci 31 14721 PMID: 21994388

Zschenderlein et al (2011) Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1. PLoS One 6 e16116 PMID: 21249195

Goldberg et al (2011) Rapid developmental maturation of neocortical FS cell intrinsic excitability. Front Cell Neurosci 21 666 PMID: 20705896

Allen et al (2011) SK2 channels are neuroprotective for ischemia-induced neuronal cell death. J Neurosci 31 2302 PMID: 21712833

Austgen et al (2011) Hydrogen sulfide augments synaptic neurotransmission in the nucleus of the solitary tract. J Neurophysiol 106 1822 PMID: 21734104

Biase et al (2011) NMDA receptor signaling in oligodendrocyte progenitors is not required for oligodendrogenesis and myelination. J Neurophysiol 31 12650 PMID: 21880926

Wei et al (2011) Development of asymmetric inhibition underlying direction selectivity in the retina. J Neurophysiol 469 402 PMID: 21131947

Torborg et al (2010) Control of CA3 output by feedforward inhibition despite developmental changes in the excitation-inhibition balance. J Neurosci 30 15628 PMID: 21084618

Person and Raman (2010) Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei. Neuron 66 550 PMID: 20510859

Kim and Alger (2010) Reduction in endocannabinoid tone is a homeostatic mechanism for specific inhibitory synapses. Nat Neurosci 13 592 PMID: 20348918

Nikolenko et al (2010) A portable laser photostimulation and imaging microscope. J Neural Eng 7 45001 PMID: 20644244

Tani et al (2010) Glutamine is required for persistent epileptiform activity in the disinhibited neocortical brain slice. J Neurosci 30 1288 PMID: 20107056

Venkataramani and Taylor (2010) Orientation selectivity in rabbit retinal ganglion cells is mediated by presynaptic inhibition. J Neurosci 30 15664 PMID: 21084622

Biase et al (2010) Excitability and synaptic communication within the oligodendrocyte lineage. J Neurosci 30 3600 PMID: 20219994

Noh et al (2010) Glutamate co-release at GABA/glycinergic synapses is crucial for the refinement of an inhibitory map. PLoS One 13 232 PMID: 20081852

Mapelli et al (2010) High-Pass Filtering and Dynamic Gain Regulation Enhance Vertical Bursts Transmission along the Mossy Fiber Pathway of Cerebellum. Nature 4 14 PMID: 20577586

Oh et al (2010) Substitution of 5-HT1A receptor signaling by a light-activated G protein-coupled receptor. Front Neural Circuits 285 30825 PMID: 20643652

Brozoski et al (2009) Differential endocannabinoid regulation of baroreflex-evoked sympathoinhibition in normotensive versus hypertensive rats. Auton Neurosci 150 82 PMID: 19464961

Babu et al (2009) Synaptic network activity induces neuronal differentiation of adult hippocampal precursor cells through BDNF signaling. Front Neurosci 3 49 PMID: 20582276

Shiratsuchi et al (2009) Propofol inhibits pressure-stimulated macrophage phagocytosis via the GABAA receptor and dysregulation of p130cas phosphorylation. Am J Physiol Cell Physiol 296 C1400 PMID: 19357231

Chuhma et al (2009) Dopamine neuron glutamate cotransmission: frequency-dependent modulation in the mesoventromedial projection. Neuroscience 164 1068 PMID: 19729052

Li et al (2009) Activity-dependent modulation of glutamatergic signaling in the developing rat dorsal horn by early tissue injury. Cereb Cortex 102 2208 PMID: 19675290

Wood et al (2009) Synaptic circuit abnormalities of motor-frontal layer 2/3 pyramidal neurons in an RNA interference model of methyl-CpG-binding protein 2 deficiency. Chem Senses 29 12440 PMID: 19812320

Fanselow et al (2008) Selective, state-dependent activation of somatostatin-expressing inhibitory interneurons in mouse neocortex. J Neurophysiol 100 2640 PMID: 18799598

Kim and Tsien (2008) Synapse-specific adaptations to inactivity in hippocampal circuits achieve homeostatic gain control while dampening network reverberation. Neuron 58 925 PMID: 18579082

Shin et al (2008) Dendritic glutamate release produces autocrine activation of mGluR1 in cerebellar Purkinje cells. J Neurosci 105 746 PMID: 18174329

Kotak et al (2008) Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex. Cereb Cortex 18 2098 PMID: 18222937

Maher and Westbrook (2008) Co-transmission of dopamine and GABA in periglomerular cells. J Neurophysiol 99 1559 PMID: 18216231

Darbin and Wichmann (2008) Effects of striatal GABA A-receptor blockade on striatal and cortical activity in monkeys. Front Cell Neurosci 99 1294 PMID: 18216224

Ziskin et al (2007) Vesicular release of glutamate from unmyelinated axons in white matter. Front Integr Neurosci 10 321 PMID: 17293857

Young and Sun (2007) Long-term modifications in the strength of excitatory associative inputs in the piriform cortex. Neuron 32 783 PMID: 17634388

Fortin and Levine (2007) Differential effects of endocannabinoids on glutamatergic and GABAergic inputs to layer 5 pyramidal neurons. Development 17 163 PMID: 16467564

Ince-Dunn et al (2006) Regulation of thalamocortical patterning and synaptic maturation by NeuroD2. Neuron 49 683 PMID: 16504944

Singh et al (2006) Altered balance of glutamatergic/GABAergic synaptic input and associated changes in dendrite morphology after BDNF expression in BDNF-deficient hippocampal neurons. Nature 26 7189 PMID: 16822976

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Ying and Goldstein (2005) Propofol suppresses synaptic responsiveness of somatosensory relay neurons to excitatory input by potentiating GABA(A) receptor chloride channels. J Neurosci 1 2 PMID: 15813991

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