MW 380.25 Da, Purity >98%. Water soluble, potent, selective and competitive AMPA/kainate receptor antagonist. Neuroprotective and anticonvulsant in vivo.
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- Nature neuroscience 27:484-4962024The developmental timing of spinal touch processing alterations predicts behavioral changes in genetic mouse models of autism spectrum disorders.Applications:Unspecified applicationReactive species:Unspecified reactive speciesAniqa Tasnim,Ilayda Alkislar,Richard Hakim,Josef Turecek,Amira Abdelaziz,Lauren L Orefice,David D GintyPubMed 38233682
- eLife 12:2023Neuropeptide Y-expressing dorsal horn inhibitory interneurons gate spinal pain and itch signalling.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKieran A Boyle,Erika Polgar,Maria Gutierrez-Mecinas,Allen C Dickie,Andrew H Cooper,Andrew M Bell,Evelline Jumolea,Adrian Casas-Benito,Masahiko Watanabe,David I Hughes,Gregory A Weir,John S Riddell,Andrew J ToddPubMed 37490401
- Cell reports 40:1114402022Dopamine D2 receptors bidirectionally regulate striatal enkephalin expression: Implications for cocaine reward.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKathy Z Dai,In Bae Choi,Ryan Levitt,Mariah B Blegen,Alanna R Kaplan,Aya Matsui,J Hoon Shin,Miriam E Bocarsly,Eleanor H Simpson,Christoph Kellendonk,Veronica A Alvarez,Lauren K DobbsPubMed 36170833
- Frontiers in neuroscience 16:9610422022Brainstem activation of GABA receptors in the nucleus tractus solitarius increases gastric motility.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLorenza Bellusci,Elizabeth Kim,Selena Garcia DuBar,Richard A Gillis,Stefano Vicini,Niaz SahibzadaPubMed 35983226
- Neuron 110:2588-2606.e62022Presynaptic FMRP and local protein synthesis support structural and functional plasticity of glutamatergic axon terminals.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHannah R Monday,Shivani C Kharod,Young J Yoon,Robert H Singer,Pablo E CastilloPubMed 35728596
- The Journal of neuroscience : the official journal of the Society for Neuroscience 42:5212-52282022Interactions between Brainstem Neurons That Regulate the Motility to the Stomach.Applications:Unspecified applicationReactive species:Unspecified reactive speciesLorenza Bellusci,Selena N Garcia DuBar,Michelle Kuah,David Castellano,Vinona Muralidaran,Elizabeth Jones,Aaron M Rozeboom,Richard A Gillis,Stefano Vicini,Niaz SahibzadaPubMed 35610046
- Cell reports 39:1107952022Serotonin receptors contribute to dopamine depression of lateral inhibition in the nucleus accumbens.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDennis A Burke,Veronica A AlvarezPubMed 35545050
- Cell 185:1943-1959.e212022PAAN/MIF nuclease inhibition prevents neurodegeneration in Parkinson's disease.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHyejin Park,Tae-In Kam,Hanjing Peng,Shih-Ching Chou,Amir A Mehrabani-Tabari,Jae-Jin Song,Xiling Yin,Senthilkumar S Karuppagounder,George K Umanah,A V Subba Rao,YuRee Choi,Akanksha Aggarwal,Sohyun Chang,Hyunhee Kim,Jiyoung Byun,Jun O Liu,Ted M Dawson,Valina L DawsonPubMed 35545089
- Current protocols 2:e4092022Experimental Protocols and Analytical Procedures for Studying Synaptic Transmission in Rodent Spinal Cord Dorsal Horn.Applications:Unspecified applicationReactive species:Unspecified reactive speciesRita BardoniPubMed 35435326
- Communications biology 5:332022Selective control of synaptically-connected circuit elements by all-optical synapses.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMansi Prakash,Jeremy Murphy,Robyn St Laurent,Nina Friedman,Emmanuel L Crespo,Andreas Bjorefeldt,Akash Pal,Yuvraj Bhagat,Julie A Kauer,Nathan C Shaner,Diane Lipscombe,Christopher I Moore,Ute HochgeschwenderPubMed 35017641
Key facts
- CAS number
- 479347-86-9
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 380.25 Da
- Molecular formula
- C12H6N4Na2O6S
- PubChem identifier
- 3272523
- Nature
- Synthetic
Alternative names
AMPA 1, AMPA-selective glutamate receptor 1, GLUH1, GRIA1_HUMAN, GluA1, GluR-1, GluR-A, GluR-K1, Glutamate receptor 1, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, HBGR1, MGC133252, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243
Recommended products
MW 380.25 Da, Purity >98%. Water soluble, potent, selective and competitive AMPA/kainate receptor antagonist. Neuroprotective and anticonvulsant in vivo.
Key facts
- CAS number
- 479347-86-9
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 380.25 Da
- Molecular formula
- C12H6N4Na2O6S
- PubChem identifier
- 3272523
- Nature
- Synthetic
- Biochemical name
- 6-Nitro-7-sulfamoylbenzo[f]quinoxaline-2,3-dione, Disodium Salt
- Biological description
Water soluble, potent, selective and competitive AMPA/kainate receptor antagonist. Neuroprotective and anticonvulsant in vivo.
- Canonical SMILES
- C1=CC2=C3C(=CC(=C2C(=C1)S(=O)(=O)N)[N+](=O)[O-])N=C(C(=N3)[O-])[O-].[Na+].[Na+]
- InChI
- InChI=1S/C12H8N4O6S.2Na/c13-23(21,22)8-3-1-2-5-9(8)7(16(19)20)4-6-10(5)15-12(18)11(17)14-6;;/h1-4H,(H,14,17)(H,15,18)(H2,13,21,22);;/q;2*+1/p-2
- InChIKey
- SVJKYIUJRJEABK-UHFFFAOYSA-L
- IUPAC name
- disodium;6-nitro-7-sulfamoylbenzo[f]quinoxaline-2,3-diolate
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Glutamate Receptor 1 (AMPA subtype) also known as GluR1 is a subunit of the AMPA receptor complex which mediates fast synaptic transmission in the central nervous system. It is an ionotropic receptor for glutamate functioning by opening ion channels to allow the flow of Na+ and Ca2+ ions across the cell membrane contributing to excitatory neurotransmission. The GluR1 subunit has a molecular mass of approximately 100 kDa. This receptor is commonly expressed in the brain regions such as the hippocampus and the cerebral cortex playing an important role in synaptic plasticity and memory formation.
- Biological function summary
The GluR1 subunit is an essential component of the AMPA receptor complex which typically forms as a tetramer. This complex modulates synaptic strength and plasticity processes critical for learning and memory. The activity of AMPA receptors including those containing GluR1 is regulated by several auxiliary proteins and is essential for post-synaptic responses. The GluR1 subunit also interacts with other proteins such as TARPs which modulate its trafficking and channel properties.
- Pathways
The GluR1-containing AMPA receptors participate significantly in the glutamatergic signaling pathway which is vital for fast excitatory synaptic transmission in the brain. This pathway also involves the NMDA receptors which work together with AMPA receptors to regulate synaptic plasticity and neuronal communication. Additionally the GluR1 interacts within the long-term potentiation (LTP) pathway contributing to the strengthening of synapses an essential mechanism underlying learning and memory.
- Associated diseases and disorders
Dysfunction in GluR1 and associated AMPA receptors has been implicated in conditions like Alzheimer's disease and epilepsy. Alzheimer's disease exhibits decreased synaptic transmission and plasticity linked to impaired GluR1 function and its interactions with NMDA receptors. In epilepsy abnormal GluR1 activity may contribute to heightened neuronal excitability and seizure propagation. Targeting GluR1 or associated pathways offers potential for therapeutic interventions in these disorders possibly through drugs such as memantine and NBQX which modulate receptor activity.
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2 product images
Chemical Structure - NBQX disodium salt, AMPA / kainate antagonist (ab120046)
2D chemical structure image of ab120046, NBQX disodium salt, AMPA / kainate antagonist
Functional Studies - NBQX disodium salt, AMPA / kainate antagonist (ab120046)
Anti-MEK1 (phospho S298) antibody [EPR3338] ab96379 staining MEK1 (phospho S298) in SK-N-SH cells treated with NBQX disodium salt (ab120046), by ICC/IF. Decrease in MEK1 (phospho S298) expression correlates with increased concentration of NBQX disodium salt, as described in literature.
The cells were incubated at 37°C for 24h in media containing different concentrations of ab120046 (NBQX disodium salt) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with Anti-MEK1 (phospho S298) antibody [EPR3338] ab96379 (1/100 dilution) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody.
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