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Non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for GluN2B (formally NR2B)- over GluN2A (NR2A)- and GluN2C (NR2C)-containing receptors (IC50 values are 1, > 100 and > 100 μM respectively). Also σ1 ligand (Ki = 0.013 μM). Antagonizes neuronal voltage-gated Ca2+ channels and selectively inhibits the rapid component of the delayed rectifier K+ current (IKr). Neuroprotective.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 347.86. 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|
|0.25 mM||11.5 mL||57.49 mL||114.99 mL|
|1.25 mM||2.3 mL||11.5 mL||23 mL|
|2.5 mM||1.15 mL||5.75 mL||11.5 mL|
|12.5 mM||0.23 mL||1.15 mL||2.3 mL|
References are publications that support the biological activity of the product.
Bath et al (1996) The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur.J.Pharmacol. 299 103 PMID: 8901012
Whittemore et al (1997) Antagonism of N-MthD.-aspartate receptors by σ site ligands: potency, subtype-selectivity and mechanisms of inhibition. J.Pharmacol.Exp.Ther. 282 326 PMID: 9223571
Lengyel et al (2004) Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br.J.Pharmacol. 143 152 PMID: 15302678
If you know of a relevant reference for Eliprodil, please let us know.
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Keywords: Eliprodil, Eliprodil supplier, σ, sigma, ligands, σ1, sigma1, σ2, sigma2, polyamine, site, NMDA, antagonists, Ca2+, channel, blockers, Neuroprotective, Non-competitive, NR2B-selective, Receptors, Glutamate, N-Methyl-D-Aspartate, iGluR, Ionotropic, GluN2B, Sigma1, 2195, Tocris Bioscience
2 Citations for Eliprodil
Citations are publications that use Tocris products. Selected citations for Eliprodil include:
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
Do you know of a great paper that uses Eliprodil from Tocris? Please let us know.
Reviews for Eliprodil
Average Rating: 5 (Based on 1 Review.)
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We studied the histological assessment of the volume of the traumatic brain lesion to estimate the extent of the structural damage. In the study, we have used this approach to evaluate the efficacity and the window of therapeutic opportunity of Eliprodil.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.