Ro 25-6981 maleate

Cat. No. 1594

Ro 25-6981 maleate C22H29NO2.C4H4O4 [1312991-76-6]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Kosowski and Liljequist (2004) 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 dopamine release in the nucleus accumbens. J.Pharmacol.Exp.Ther. 311 560. PMID: 15256539.

Lynch et al (2001) Pharmacological characterization of interactions of RO 25-6981 with the NR2B (ε2) subunit. Eur.J.Pharmacol. 416 185. PMID: 11290368.

Fischer et al (1997) Ro 25-6981, a highly potent and selective blocker of N-Methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro. J.Pharmacol.Exp.Ther. 283 1285. PMID: 9400004.

If you know of a relevant reference for this product please let us know.

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

Chen et al (2016) β-arrestin-2 regulates NMDA receptor function in spinal lamina II neurons and duration of persistent pain. Nature Communications 7 12531. PMID: 27538456.

Volkmann et al (2016) MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit. PLoS One 11 e0148129. PMID: 26829109.

Lauderdale et al (2015) Osmotic Edema Rapidly Increases Neuronal Excitability Through Activation of NMDA Receptor-Dependent Slow Inward Currents in Juvenile and Adult Hippocampus. ASN Neuro 7. PMID: 26489684.

Tindi et al (2015) ANKS1B Gene Product AIDA-1 Controls Hippocampal Synaptic Transmission by Regulating GluN2B Subunit Localization. J Neurosci 35 8986. PMID: 26085624.

Smith et al (2014) A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation. Mol Pharmacol 86 390. PMID: 25057049.

Hamida et al (2013) Protein tyrosine phosphatase α in the dorsomedial striatum promotes excessive ethanol-drinking behaviors. Transl Psychiatry 33 14369. PMID: 24005290.

Louderback et al (2013) Knockdown of BNST GluN2B-containing NMDA receptors mimics the actions of ketamine on novelty-induced hypophagia. Psychoneuroendocrinology 3 e331. PMID: 24301649.

Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase. Sci Rep 3 926. PMID: 23378895.

Urban et al (2013) Treatment with a clinically-relevant dose of methylphenidate alters NMDA receptor composition and synaptic plasticity in the juvenile rat prefrontal cortex. Mol Brain 101 65. PMID: 23333502.

Bortolato et al (2012) NMDARs mediate the role of monoamine oxidase A in pathological aggression. J Neurosci 32 8574. PMID: 22723698.

Hoshiko et al (2012) Deficiency of the microglial receptor CX3CR1 impairs postnatal functional development of thalamocortical synapses in the barrel cortex. J Neurosci 32 15106. PMID: 23100431.

Ishima and Hashimoto (2012) Potentiation of nerve growth factor-induced neurite outgrowth in PC12 cells by ifenprodil: the role of σ-1 and IP3 receptors. Neurobiol Learn Mem 7 e37989. PMID: 22655093.

Nebieridze et al (2012) β-Estradiol unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus. PLoS One 37 1845. PMID: 22541715.

Olsen and Sheng (2012) NMDA receptors and BAX are essential for Aβ impairment of LTP. Sci Rep 2 225. PMID: 22355739.

Noel et al (2011) Tissue plasminogen activator is required for the development of fetal alcohol syndrome in mice. Proc Natl Acad Sci U S A 108 5069. PMID: 21383198.

Xie et al (2011) Dependence of NMDA/GSK-3β mediated metaplasticity on TRPM2 channels at hippocampal CA3-CA1 synapses. J Neurosci 4 44. PMID: 22188973.

Terasaki et al (2010) Activation of NR2A receptors induces ischemic tolerance through CREB signaling. J Cereb Blood Flow Metab 30 1441. PMID: 20145658.

Beazely et al (2009) Platelet-derived growth factor selectively inhibits NR2B-containing N-methyl-D-aspartate receptors in CA1 hippocampal neurons. J Biol Chem 284 8054. PMID: 19106110.

Hellier et al (2009) NMDA receptor-mediated long-term alterations in epileptiform activity in experimental chronic epilepsy. Neuropharmacology 56 414. PMID: 18930747.

Popp et al (2008) Cerebellar granule cells cultured from adolescent rats express functional NMDA receptors: an in vitro model for studying the developing cerebellum. J Neurochem 106 900. PMID: 18466339.

Ge et al (2007) A critical period for enhanced synaptic plasticity in newly generated neurons of the adult brain. Neuron 54 559. PMID: 17521569.

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