SR 95531 hydrobromide

Cat. No. 1262

SR 95531 hydrobromide C15H17N3O3.HBr [104104-50-9]

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Alternative Name: 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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

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.

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.

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.

If you know of a relevant reference for this product please let us know.

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

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.

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

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.

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

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.

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

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.

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.

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

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

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.

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.

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

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

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

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

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

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.

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

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.

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.

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

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.

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

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

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.

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.

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

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.

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

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.

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

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

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.

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.

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

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.

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

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

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

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

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.

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.

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

Foeller et al (2005) Inhibitory sharpening of receptive fields contributes to whisker map plasticity in rat somatosensory cortex. J Neurophysiol 94 4387. PMID: 16162832.

Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551. PMID: 15140926.

Labrakakis et al (2003) Localization and function of ATP and GABAA receptors expressed by nociceptors and other postnatal sensory neurons in rat. J Physiol 549 131. PMID: 12665615.

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Keywords: SR 95531 hydrobromide, supplier, Selective, competitive, GABAA, receptor, antagonists, Receptors, SR95531, hydrobromide, Tocris Bioscience, GABAA Receptor Antagonist products

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