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Ro 25-6981 maleate

Catalog #: 1594
29 Citations Datasheet / COA / SDS
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1594/50
1594/1
Ro 25-6981 maleate | CAS No. 1312991-76-6 | NMDA Receptor Antagonists
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Description: GluN2B-selective NMDA antagonist

Chemical Name: (αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate

Purity: ≥98%

Product Details
Citations (29)
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Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Ro 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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Stress hormone rapidly tunes synaptic NMDA receptor through membrane dynamics and mineralocorticoid signalling
    L Mikasova, H Xiong, A Kerkhofs, D Bouchet, HJ Krugers, L Groc
    Sci Rep, 2017;7(1):8053.
  2. MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit.
    Volkmann R, Fanger C, Anderson D, Sirivolu V, Paschetto K, Gordon E, Virginio C, Gleyzes M, Buisson B, Steidl E, Mierau S, Fagiolini M, Menniti F
    PLoS ONE, 2016;11(2):e0148129.
  3. Rapid synaptic potentiation within the anterior cingulate cortex mediates trace fear learning.

    Mol Brain, 2012;5(0):6.
  4. Contribution of astroglial Cx43 hemichannels to the modulation of glutamatergic currents by D-serine in the mouse prefrontal cortex
    C Meunier, N Wang, C Yi, G Dallerac, P Ezan, A Koulakoff, L Leybaert, C Giaume
    J. Neurosci., 2017;0(0):.
  5. Potentiation of nerve growth factor-induced neurite outgrowth in PC12 cells by ifenprodil: the role of sigma-1 and IP3 receptors.
    Ishima T, Hashimoto K
    PLoS ONE, 2012;7(5):e37989.
  6. Potentiation of Synaptic GluN2B NMDAR Currents by Fyn Kinase Is Gated through BDNF-Mediated Disinhibition in Spinal Pain Processing

    Cell Rep, 2016;17(10):2753-2765.
  7. Ro 25-6981, a highly potent and selective blocker of N-MthD.-aspartate receptors containing the NR2B subunit. Characterization in vitro.
    Fischer et al.
    J.Pharmacol.Exp.Ther., 1997;283:1285
  8. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (ε2) subunit.
    Lynch et al.
    Eur.J.Pharmacol., 2001;416:185
  9. 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
    J.Pharmacol.Exp.Ther., 2004;311:560
  10. Hevin/Sparcl1 drives pathological pain through spinal cord astrocyte and NMDA receptor signaling
    G Chen, J Xu, H Luo, X Luo, SK Singh, JJ Ramirez, ML James, JP Mathew, M Berger, C Eroglu, RR Ji
    JCI Insight, 2022;7(23):.

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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

  1. 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
  2. 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
  3. Multiple roles of GluN2B-containing NMDA receptors in synaptic plasticity in juvenile hippocampus.
    Authors: France
    Neuropharmacology  2017;112:76
  4. 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
  5. 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
  6. 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
  7. 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
  8. ANKS1B Gene Product AIDA-1 Controls Hippocampal Synaptic Transmission by Regulating GluN2B Subunit Localization.
    Authors: Tindi Et al.
    J Neurosci  2015;35:8986
  9. 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
  10. The role of GluN2A and GluN2B subunits on the effects of NMDA receptor antagonists in modeling schizophrenia and treating refractory depression.
    Authors: Jim&eacutenez-Sánchez Et al.
    Neuropsychopharmacology  2014;39:2673
  11. Impaired glutamate recycling and GluN2B-mediated neuronal calcium overload in mice lacking TGF-β1 in the CNS.
    Authors: Koeglsperger Et al.
    Glia  2013;61:985
  12. Knockdown of BNST GluN2B-containing NMDA receptors mimics the actions of KA on novelty-induced hypophagia.
    Authors: Louderback Et al.
    Psychoneuroendocrinology  2013;3:e331
  13. Group II metabotropic glutamate receptors modify N-MthD.-aspartate receptors via Src kinase.
    Authors: Trepanier Et al.
    Sci Rep  2013;3:926
  14. Protein tyrosine phosphatase α in the dorsomedial striatum promotes excessive ethanol-drinking behaviors.
    Authors: Hamida Et al.
    Transl Psychiatry  2013;33:14369
  15. Long-term potentiation of synaptic transmission in the adult mouse insular cortex: multielectrode array recordings.
    Authors: Liu Et al.
    J Neurophysiol  2013;110:505
  16. 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
  17. 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
  18. 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
  19. NMDARs mediate the role of monoamine oxidase A in pathological aggression.
    Authors: Bortolato Et al.
    J Neurosci  2012;32:8574
  20. 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
  21. NMDA receptors and BAX are essential for Aβ impairment of LTP.
    Authors: Olsen and Sheng
    Sci Rep  2012;2:225
  22. Dependence of NMDA/GSK-3β mediated metaplasticity on TRPM2 channels at hippocampal CA3-CA1 synapses.
    Authors: Xie Et al.
    J Neurosci  2011;4:44
  23. 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
  24. Activation of NR2A receptors induces ischemic tolerance through CREB signaling.
    Authors: Terasaki Et al.
    J Cereb Blood Flow Metab  2010;30:1441
  25. NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy.
    Authors: Hellier Et al.
    Neuropharmacology  2009;56:414
  26. 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
  27. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.
    Authors: Niswender Et al.
    Mol Pharmacol  2008;74:1345
  28. 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
  29. A critical period for enhanced synaptic plasticity in newly generated neurons of the adult brain.
    Authors: Ge Et al.
    Neuron  2007;54:559

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