Abcam, ab120290, Ro 25-6981 maleate salt, NR2B antagonist

Size: 1mg / 10mg / 50mg
MW 455.5 Da. Potent, highly selective, activity-dependent blocker of NMDA receptors that contain the NR2B subunit (IC 50 values are 0.009 and 52 μM at NR1C/NR2B and NR1C/NR2A, respectively). Displays no significant activity at kainate/AMPA receptors, Na + and Ca 2+ channels at concentrations showing maximal protection in neurotoxicity tests. Neuroprotective actions in vivo and in vitro .
Key facts
CAS number:1312991-76-6,
Form:SolidSee storage information,
Molecular weight:455.5 Da,
Molecular formula:C26H33NO6,
PubChem: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

Properties and Storage Information:
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 Information:
This supplementary information is collated from multiple sources and compiled automatically.
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.
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.