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AB120290

Ro 25-6981 maleate salt, NR2B antagonist

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(9 Publications)

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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Functional Studies - Ro 25-6981 maleate salt, NR2B antagonist (AB120290)
  • FuncS

PubMed

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.

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.

Chemical Structure - Ro 25-6981 maleate salt, NR2B antagonist (AB120290)
  • Chemical Structure

Lab

Chemical Structure - Ro 25-6981 maleate salt, NR2B antagonist (AB120290)

2D chemical structure image of ab120290, Ro 25-6981 maleate salt, NR2B antagonist

Key facts

CAS number

1312991-76-6

Form

Solid

form

Molecular weight

455.5 Da

Molecular formula

C<sub>2</sub><sub>6</sub>H<sub>3</sub><sub>3</sub>NO<sub>6</sub>

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

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Biochemicals

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Secondary Antibodies

AB150113

Goat Anti-Mouse IgG H&L (Alexa Fluor® 488)

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Biochemicals

AB120045

NBQX, AMPA / kainate antagonist

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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
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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.
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Product protocols

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Publications (9)

Recent publications for all applications. Explore the full list and refine your search

Neuron 108:919-936.e11 PubMed32976770

2020

LTP Induction Boosts Glutamate Spillover by Driving Withdrawal of Perisynaptic Astroglia.

Applications

Unspecified application

Species

Unspecified reactive species

Christian Henneberger,Lucie Bard,Aude Panatier,James P Reynolds,Olga Kopach,Nikolay I Medvedev,Daniel Minge,Michel K Herde,Stefanie Anders,Igor Kraev,Janosch P Heller,Sylvain Rama,Kaiyu Zheng,Thomas P Jensen,Inmaculada Sanchez-Romero,Colin J Jackson,Harald Janovjak,Ole Petter Ottersen,Erlend Arnulf Nagelhus,Stephane H R Oliet,Michael G Stewart,U Valentin Nägerl,Dmitri A Rusakov

The Journal of neuroscience : the official journal of the Society for Neuroscience 33:19534-54 PubMed24336719

2013

Dysfunctional 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 application

Species

Unspecified reactive species

Benjamin G Gunn,Linda Cunningham,Michelle A Cooper,Nicole L Corteen,Mohsen Seifi,Jerome D Swinny,Jeremy J Lambert,Delia Belelli

Alcohol (Fayetteville, N.Y.) 47:531-7 PubMed24103431

2013

Developmental changes in the acute ethanol sensitivity of glutamatergic and GABAergic transmission in the BNST.

Applications

Unspecified application

Species

Unspecified reactive species

T A Wills,T L Kash,D G Winder

Biological psychiatry 76:387-96 PubMed24094509

2013

The dyslexia-associated gene DCDC2 is required for spike-timing precision in mouse neocortex.

Applications

Unspecified application

Species

Unspecified reactive species

Alicia Che,Matthew J Girgenti,Joseph LoTurco

The Journal of physiology 591:1809-22 PubMed23339172

2013

Input-specific learning rules at excitatory synapses onto hippocampal parvalbumin-expressing interneurons.

Applications

Unspecified application

Species

Unspecified reactive species

Nicolas Le Roux,Carolina Cabezas,Urs Lucas Böhm,Jean Christophe Poncer

The Journal of biological chemistry 287:25073-85 PubMed22679016

2012

Chronic opioid potentiates presynaptic but impairs postsynaptic N-methyl-D-aspartic acid receptor activity in spinal cords: implications for opioid hyperalgesia and tolerance.

Applications

Unspecified application

Species

Unspecified reactive species

Yi-Lin Zhao,Shao-Rui Chen,Hong Chen,Hui-Lin Pan

The Journal of biological chemistry 287:17438-46 PubMed22474321

2012

Casein kinase 2-mediated synaptic GluN2A up-regulation increases N-methyl-D-aspartate receptor activity and excitability of hypothalamic neurons in hypertension.

Applications

Unspecified application

Species

Unspecified reactive species

Zeng-You Ye,Li Li,De-Pei Li,Hui-Lin Pan

Proceedings of the National Academy of Sciences of 109:E278-87 PubMed22219357

2012

GluN2B subunit deletion reveals key role in acute and chronic ethanol sensitivity of glutamate synapses in bed nucleus of the stria terminalis.

Applications

Unspecified application

Species

Unspecified reactive species

Tiffany A Wills,Jason R Klug,Yuval Silberman,Anthony J Baucum,Carl Weitlauf,Roger J Colbran,Eric Delpire,Danny G Winder

Neuroscience 199:51-63 PubMed22027237

2011

Complex receptor mediation of acute ketamine application on in vitro gamma oscillations in mouse prefrontal cortex: modeling gamma band oscillation abnormalities in schizophrenia.

Applications

Unspecified application

Species

Unspecified reactive species

J M McNally,R W McCarley,J T McKenna,Y Yanagawa,R E Brown
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