MW 455.5 Da. Potent, highly selective, activity-dependent blocker of NMDA receptors that contain the NR2B subunit (IC50 values are 0.009 and 52 μM at NR1C/NR2B and NR1C/NR2A, respectively). Displays no significant activity at kainate/AMPA receptors, Na+ and Ca2+ channels at concentrations showing maximal protection in neurotoxicity tests. Neuroprotective actions in vivo and in vitro.
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- Neuron 108:919-936.e112020LTP Induction Boosts Glutamate Spillover by Driving Withdrawal of Perisynaptic Astroglia.Applications:Unspecified applicationReactive species:Unspecified reactive speciesChristian Henneberger et. al.PubMed 32976770
- The Journal of neuroscience : the official journal of the Society for Neuroscience 33:19534-542013Dysfunctional astrocytic and synaptic regulation of hypothalamic glutamatergic transmission in a mouse model of early-life adversity: relevance to neurosteroids and programming of the stress response.Applications:Unspecified applicationReactive species:Unspecified reactive speciesBenjamin G Gunn,Linda Cunningham,Michelle A Cooper,Nicole L Corteen,Mohsen Seifi,Jerome D Swinny,Jeremy J Lambert,Delia BelelliPubMed 24336719
- Alcohol (Fayetteville, N.Y.) 47:531-72013Developmental changes in the acute ethanol sensitivity of glutamatergic and GABAergic transmission in the BNST.Applications:Unspecified applicationReactive species:Unspecified reactive speciesT A Wills et. al.PubMed 24103431
- Biological psychiatry 76:387-962013The dyslexia-associated gene DCDC2 is required for spike-timing precision in mouse neocortex.Applications:Unspecified applicationReactive species:Unspecified reactive speciesAlicia Che et. al.PubMed 24094509
- The Journal of physiology 591:1809-222013Input-specific learning rules at excitatory synapses onto hippocampal parvalbumin-expressing interneurons.Applications:Unspecified applicationReactive species:Unspecified reactive speciesNicolas Le Roux et. al.PubMed 23339172
- The Journal of biological chemistry 287:25073-852012Chronic opioid potentiates presynaptic but impairs postsynaptic N-methyl-D-aspartic acid receptor activity in spinal cords: implications for opioid hyperalgesia and tolerance.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYi-Lin Zhao et. al.PubMed 22679016
- The Journal of biological chemistry 287:17438-462012Casein kinase 2-mediated synaptic GluN2A up-regulation increases N-methyl-D-aspartate receptor activity and excitability of hypothalamic neurons in hypertension.Applications:Unspecified applicationReactive species:Unspecified reactive speciesZeng-You Ye et. al.PubMed 22474321
- Proceedings of the National Academy of Sciences of 109:E278-872012GluN2B subunit deletion reveals key role in acute and chronic ethanol sensitivity of glutamate synapses in bed nucleus of the stria terminalis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTiffany A Wills et. al.PubMed 22219357
- Neuroscience 199:51-632011Complex receptor mediation of acute ketamine application on in vitro gamma oscillations in mouse prefrontal cortex: modeling gamma band oscillation abnormalities in schizophrenia.Applications:Unspecified applicationReactive species:Unspecified reactive speciesJ M McNally et. al.PubMed 22027237
Key facts
- CAS number
- 1312991-76-6
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 455.5 Da
- Molecular formula
- C26H33NO6
- PubChem identifier
- 53250677
- 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
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MW 455.5 Da. Potent, highly selective, activity-dependent blocker of NMDA receptors that contain the NR2B subunit (IC50 values are 0.009 and 52 μM at NR1C/NR2B and NR1C/NR2A, respectively). Displays no significant activity at kainate/AMPA receptors, Na+ and Ca2+ channels at concentrations showing maximal protection in neurotoxicity tests. Neuroprotective actions in vivo and in vitro.
Key facts
- CAS number
- 1312991-76-6
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 455.5 Da
- Molecular formula
- C26H33NO6
- PubChem identifier
- 53250677
- Nature
- Synthetic
- Biochemical name
- Ro 25-6981 maleate
- Biological description
Potent, highly selective, activity-dependent blocker of NMDA receptors that contain the NR2B subunit (IC50 values are 0.009 and 52 μM at NR1C/NR2B and NR1C/NR2A, respectively). Displays no significant activity at kainate/AMPA receptors, Na+ and Ca2+ channels at concentrations showing maximal protection in neurotoxicity tests. Neuroprotective actions in vivo and in vitro.
- Canonical SMILES
- CC(CN1CCC(CC1)CC2=CC=CC=C2)C(C3=CC=C(C=C3)O)O.C(=CC(=O)O)C(=O)O
- Isomeric SMILES
- C[C@@H](CN1CCC(CC1)CC2=CC=CC=C2)[C@H](C3=CC=C(C=C3)O)O.C(=C\C(=O)O)\C(=O)O
- InChI
- InChI=1S/C22H29NO2.C4H4O4/c1-17(22(25)20-7-9-21(24)10-8-20)16-23-13-11-19(12-14-23)15-18-5-3-2-4-6-18;5-3(6)1-2-4(7)8/h2-10,17,19,22,24-25H,11-16H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t17-,22+;/m0./s1
- InChIKey
- FYJZEHCQSUBZDY-SEELMCCHSA-N
- IUPAC name
- 4-[(1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol;(Z)-but-2-enedioic acid
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- 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 - Ro 25-6981 maleate salt, NR2B antagonist (ab120290)
2D chemical structure image of ab120290, Ro 25-6981 maleate salt, NR2B antagonist
Image from Wills TA et al., Proc Natl Acad Sci U S A. 2012;109(5):E278-87. Fig 6(B).; doi: 10.1073/pnas.1113820109.Functional Studies - Ro 25-6981 maleate salt, NR2B antagonist (ab120290)
Averaged time courses of NMDA receptor-isolated synaptic field potentials in dorsal lateral bed nucleus of the stria terminalis following 60 minutes of Ro 25-6981 (0.2, 2.0, or 10 μM; ab120290) in slices from naive adult male C57BL/6J mice.
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