Ro 25-6981 maleate

Pricing Availability Delivery Time Qty
Cat.No. 1594 - Ro 25-6981 maleate | C22H29NO2.C4H4O4 | CAS No. 1312991-76-6
Description: NR2B-selective NMDA antagonist
Chemical Name: (αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate
Purity: ≥98% (HPLC)
Datasheet
Citations (22)
Literature

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.

Compound Libraries

Ro 25-6981 maleate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 455.55
Formula C22H29NO2.C4H4O4
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1312991-76-6
PubChem ID 53250677
InChI Key FYJZEHCQSUBZDY-SEELMCCHSA-N
Smiles OC(=O)\C=C/C(O)=O.C[C@@H](CN1CCC(CC2=CC=CC=C2)CC1)[C@@H](O)C1=CC=C(O)C=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.55 100
water 4.56 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 455.55. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.2 mL 10.98 mL 21.95 mL
5 mM 0.44 mL 2.2 mL 4.39 mL
10 mM 0.22 mL 1.1 mL 2.2 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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 dopamin 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


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Keywords: Subtype-selective NR2B antagonists Glutamate NMDA Receptors N-Methyl-D-Aspartate iGlur Ionotropic Ro25-6981 maleate NMDA Receptors

22 Citations for Ro 25-6981 maleate

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

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

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

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

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

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

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

France (2017) Multiple roles of GluN2B-containing NMDA receptors in synaptic plasticity in juvenile hippocampus. Neuropharmacology 112 76 PMID: 27523302

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

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

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

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

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

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

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

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

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


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