Ro 25-6981 maleate
Chemical Name: (αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate
Biological ActivityRo 25-6981 maleate is a potent and selective activity-dependent blocker of NMDA receptors containing the GluN2B (formally NR2B) subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations GluN1C/GluN2B and GluN1C/GluN2A respectively. Displays neuroprotectant effects in vivo and in vitro.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Ro 25-6981, a highly potent and selective blocker of N-MthD.-aspartate receptors containing the NR2B subunit. Characterization in vitro.
Fischer et al.
Pharmacological characterization of interactions of RO 25-6981 with the NR2B (ε2) subunit.
Lynch et al.
The NR2B- selective N-MthD.-aspartate receptor antagonist Ro 25-6981 [(±)-(R*,S*)-α-(4-hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidine propanol] potentiates the effect of nicotine on locomotor activity and DA release
Kosowski and Liljequist
Citations for Ro 25-6981 maleate
The citations listed below are publications that use Tocris products. Selected citations for Ro 25-6981 maleate include:
29 Citations: Showing 1 - 10
Glutamatergic and dopaminergic modulation of cortico-striatal circuits probed by dynamic calcium imaging of networks reconstructed in microfluidic chips.
Authors: Lassus Et al.
Sci Rep 2018;8:17461
Adenylyl Cyclase 1 Is Required for Ethanol-Induced Locomotor Sensitization and Associated Increases in NMDA Receptor Phosphorylation and Function in the Dorsal Medial Striatum.
Authors: Bosse Et al.
J Pharmacol Exp Ther 2017;363:148
Multiple roles of GluN2B-containing NMDA receptors in synaptic plasticity in juvenile hippocampus.
β-arrestin-2 regulates NMDA receptor function in spinal lamina II neurons and duration of persistent pain.
Authors: Chen Et al.
Nature Communications 2016;7:12531
NR2A-Containing NMDARs in the Prefrontal Cortex Are Required for Working Memory and Associated with Age-Related Cognitive Decline.
Authors: McQuail Et al.
J Neurosci 2016;36:12537
MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit.
Authors: Volkmann Et al.
PLoS One 2016;11:e0148129
Osmotic Edema Rapidly Increases Neuronal Excitability Through Activation of NMDA Receptor-Dependent Slow Inward Currents in Juvenile and Adult Hippocampus.
Authors: Lauderdale Et al.
ASN Neuro 2015;7
ANKS1B Gene Product AIDA-1 Controls Hippocampal Synaptic Transmission by Regulating GluN2B Subunit Localization.
Authors: Tindi Et al.
J Neurosci 2015;35:8986
A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation.
Authors: Smith Et al.
Mol Pharmacol 2014;86:390
The role of GluN2A and GluN2B subunits on the effects of NMDA receptor antagonists in modeling schizophrenia and treating refractory depression.
Authors: Jiménez-Sánchez Et al.
Impaired glutamate recycling and GluN2B-mediated neuronal calcium overload in mice lacking TGF-β1 in the CNS.
Authors: Koeglsperger Et al.
Knockdown of BNST GluN2B-containing NMDA receptors mimics the actions of KA on novelty-induced hypophagia.
Authors: Louderback Et al.
Group II metabotropic glutamate receptors modify N-MthD.-aspartate receptors via Src kinase.
Authors: Trepanier Et al.
Sci Rep 2013;3:926
Protein tyrosine phosphatase α in the dorsomedial striatum promotes excessive ethanol-drinking behaviors.
Authors: Hamida Et al.
Transl Psychiatry 2013;33:14369
Long-term potentiation of synaptic transmission in the adult mouse insular cortex: multielectrode array recordings.
Authors: Liu Et al.
J Neurophysiol 2013;110:505
Treatment with a clinically-relevant dose of methylphen. alters NMDA receptor composition and synaptic plasticity in the juvenile rat prefrontal cortex.
Authors: Urban Et al.
Mol Brain 2013;101:65
Potentiation of nerve growth factor-induced neurite outgrowth in PC12 cells by ifenprodil: the role of σ-1 and IP3 receptors.
Authors: Ishima and Hashimoto
Neurobiol Learn Mem 2012;7:e37989
β-OE unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus.
Authors: Nebieridze Et al.
PLoS One 2012;37:1845
NMDARs mediate the role of monoamine oxidase A in pathological aggression.
Authors: Bortolato Et al.
J Neurosci 2012;32:8574
Deficiency of the microglial receptor CX3CR1 impairs postnatal functional development of thalamocortical synapses in the barrel cortex.
Authors: Hoshiko Et al.
J Neurosci 2012;32:15106
NMDA receptors and BAX are essential for Aβ impairment of LTP.
Authors: Olsen and Sheng
Sci Rep 2012;2:225
Dependence of NMDA/GSK-3β mediated metaplasticity on TRPM2 channels at hippocampal CA3-CA1 synapses.
Authors: Xie Et al.
J Neurosci 2011;4:44
Tissue plasminogen activator is required for the development of fetal alcohol syndrome in mice.
Authors: Noel Et al.
Proc Natl Acad Sci U S A 2011;108:5069
Activation of NR2A receptors induces ischemic tolerance through CREB signaling.
Authors: Terasaki Et al.
J Cereb Blood Flow Metab 2010;30:1441
NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy.
Authors: Hellier Et al.
Platelet-derived growth factor selectively inhibits NR2B-containing N-MthD.-aspartate receptors in CA1 hippocampal neurons.
Authors: Beazely Et al.
J Biol Chem 2009;284:8054
Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.
Authors: Niswender Et al.
Mol Pharmacol 2008;74:1345
Cerebellar granule cells cultured from adolescent rats express functional NMDA receptors: an in vitro model for studying the developing cerebellum.
Authors: Popp Et al.
J Neurochem 2008;106:900
A critical period for enhanced synaptic plasticity in newly generated neurons of the adult brain.
Authors: Ge Et al.
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