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Submit ReviewRo 25-6981 maleate
Description: GluN2B-selective NMDA antagonist
Chemical Name: (αR,βS)-α-(4-Hydroxyphenyl)-β-methyl-4-(phenylmethyl)-1-piperidinepropanol maleate
Purity: ≥98% (HPLC)
Biological Activity for Ro 25-6981 maleate
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.
Compound Libraries for Ro 25-6981 maleate
Ro 25-6981 maleate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Ro 25-6981 maleate
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ro 25-6981 maleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 4.56 | 10 with gentle warming | |
| DMSO | 45.55 | 100 |
Preparing Stock Solutions for Ro 25-6981 maleate
The following data is based on the product molecular weight 455.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for Ro 25-6981 maleate
References for Ro 25-6981 maleate
References are publications that support the biological activity of the product.
Fischer et al (1997) Ro 25-6981, a highly potent and selective blocker of N-MthD.-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-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 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
If you know of a relevant reference for Ro 25-6981 maleate, please let us know.
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Keywords: Ro 25-6981 maleate, Ro 25-6981 maleate supplier, Subtype-selective, NR2B, antagonists, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGlur, Ionotropic, Ro25-6981, maleate, GluN2B, 1594, Tocris Bioscience
29 Citations for Ro 25-6981 maleate
Citations are publications that use Tocris products. Selected citations for Ro 25-6981 maleate include:
Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-MthD.-aspartate receptors via Src kinase. Sci Rep 3 926 PMID: 23378895
France (2017) Multiple roles of GluN2B-containing NMDA receptors in synaptic plasticity in juvenile hippocampus. Neuropharmacology 112 76 PMID: 27523302
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-MthD.-aspartate receptors in CA1 hippocampal neurons. J Biol Chem 284 8054 PMID: 19106110
Bosse et al (2017) Adenylyl Cyclase 1 Is Required for Ethanol-Induced Locomotor Sensitization and Associated Increases in NMDA Receptor Phosphorylation and Function in the Dorsal Medial Striatum. J Pharmacol Exp Ther 363 148 PMID: 28838956
McQuail et al (2016) NR2A-Containing NMDARs in the Prefrontal Cortex Are Required for Working Memory and Associated with Age-Related Cognitive Decline. J Neurosci 36 12537 PMID: 27807032
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
Lassus et al (2018) Glutamatergic and dopaminergic modulation of cortico-striatal circuits probed by dynamic calcium imaging of networks reconstructed in microfluidic chips. Sci Rep 8 17461 PMID: 30498197
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
Koeglsperger et al (2013) Impaired glutamate recycling and GluN2B-mediated neuronal calcium overload in mice lacking TGF-β1 in the CNS. Glia 61 985 PMID: 23536313
Liu et al (2013) Long-term potentiation of synaptic transmission in the adult mouse insular cortex: multielectrode array recordings. J Neurophysiol 110 505 PMID: 23636718
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
Terasaki et al (2010) Activation of NR2A receptors induces ischemic tolerance through CREB signaling. J Cereb Blood Flow Metab 30 1441 PMID: 20145658
Jiménez-Sánchez et al (2014) The role of GluN2A and GluN2B subunits on the effects of NMDA receptor antagonists in modeling schizophrenia and treating refractory depression. Neuropsychopharmacology 39 2673 PMID: 24871546
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
Nebieridze et al (2012) β-OE unmasks metabotropic receptor-mediated metaplasticity of NMDA receptor transmission in the female rat dentate gyrus. PLoS One 37 1845 PMID: 22541715
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
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
Urban et al (2013) Treatment with a clinically-relevant dose of methylphen. alters NMDA receptor composition and synaptic plasticity in the juvenile rat prefrontal cortex. Mol Brain 101 65 PMID: 23333502
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 KA on novelty-induced hypophagia. Psychoneuroendocrinology 3 e331 PMID: 24301649
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
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
Niswender et al (2008) Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol 74 1345 PMID: 18664603
Ge et al (2007) A critical period for enhanced synaptic plasticity in newly generated neurons of the adult brain. Neuron 54 559 PMID: 17521569
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
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Effect of Ro 25-6981 maleate on NMDA-receptor mediated current in the basolateral amygdala following chronic ethanol exposure.
By
Anonymous on 05/10/2019
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: Basolateral Amygdala Slices
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.
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