Catalog Number: 1594
Chemical Name: (αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate
Biological Activity
Potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Displays neuroprotectant effects in vivo and in vitro.
Technical Data
  • M.Wt:
    455.55
  • Formula:
    C22H29NO2.C4H4O4
  • Solubility:
    Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    1312991-76-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Ro 25-6981, a highly potent and selective blocker of N-Methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro.
    Fischer et al.
    J.Pharmacol.Exp.Ther., 1997;283:1285
  2. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (ε2) subunit.
    Lynch et al.
    Eur.J.Pharmacol., 2001;416:185
  3. The NR2B- selective N-methyl-D-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 dopamin
    Kosowski and Liljequist
    J.Pharmacol.Exp.Ther., 2004;311:560
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Ro 25-6981 maleate include:

22 Citations: Showing 1 - 10
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  1. Multiple roles of GluN2B-containing NMDA receptors in synaptic plasticity in juvenile hippocampus.
    Authors: France
    Neuropharmacology 2017;112:76
  2. 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
  3. 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
  4. 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
  5. ANKS1B Gene Product AIDA-1 Controls Hippocampal Synaptic Transmission by Regulating GluN2B Subunit Localization.
    Authors: Tindi Et al.
    J Neurosci 2015;35:8986
  6. 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
  7. Knockdown of BNST GluN2B-containing NMDA receptors mimics the actions of ketamine on novelty-induced hypophagia.
    Authors: Louderback Et al.
    Psychoneuroendocrinology 2013;3:e331
  8. Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase.
    Authors: Trepanier Et al.
    Sci Rep 2013;3:926
  9. Protein tyrosine phosphatase α in the dorsomedial striatum promotes excessive ethanol-drinking behaviors.
    Authors: Hamida Et al.
    Transl Psychiatry 2013;33:14369
  10. Treatment with a clinically-relevant dose of methylphenidate alters NMDA receptor composition and synaptic plasticity in the juvenile rat prefrontal cortex.
    Authors: Urban Et al.
    Mol Brain 2013;101:65
  11. 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
  12. β-Estradiol unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus.
    Authors: Nebieridze Et al.
    PLoS One 2012;37:1845
  13. NMDARs mediate the role of monoamine oxidase A in pathological aggression.
    Authors: Bortolato Et al.
    J Neurosci 2012;32:8574
  14. 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
  15. NMDA receptors and BAX are essential for Aβ impairment of LTP.
    Authors: Olsen and Sheng
    Sci Rep 2012;2:225
  16. Dependence of NMDA/GSK-3β mediated metaplasticity on TRPM2 channels at hippocampal CA3-CA1 synapses.
    Authors: Xie Et al.
    J Neurosci 2011;4:44
  17. 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
  18. Activation of NR2A receptors induces ischemic tolerance through CREB signaling.
    Authors: Terasaki Et al.
    J Cereb Blood Flow Metab 2010;30:1441
  19. NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy.
    Authors: Hellier Et al.
    Neuropharmacology 2009;56:414
  20. Platelet-derived growth factor selectively inhibits NR2B-containing N-methyl-D-aspartate receptors in CA1 hippocampal neurons.
    Authors: Beazely Et al.
    J Biol Chem 2009;284:8054
  21. 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
  22. A critical period for enhanced synaptic plasticity in newly generated neurons of the adult brain.
    Authors: Ge Et al.
    Neuron 2007;54:559
Expand to show all 22 Citations

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