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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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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We used this drug to block NMDA receptors containing the GluN2B subunit on pyramidal neurons in the basolateral amygdala (BLA). We recorded from coronal sections of BLA and bath applied Ro 25-6981 maleate for 10 minutes.