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Submit ReviewEliprodil
说明： Non-competitive and GluN2B-selective NMDA antagonist
化学名： α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol
纯度： ≥98% (HPLC)
生物活性 for Eliprodil
Eliprodil is a 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.
化合物库 for Eliprodil
Eliprodil is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Eliprodil
| 分子量 | 347.86 |
| 公式 | C20H23ClFNO |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 119431-25-3 |
| PubChem ID | 60703 |
| InChI Key | GGUSQTSTQSHJAH-UHFFFAOYSA-N |
| Smiles | OC(CN1CCC(CC2=CC=C(F)C=C2)CC1)C1=CC=C(Cl)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for Eliprodil
参考文献 for Eliprodil
参考文献是支持产品生物活性的出版物。
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
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关键词: 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 篇 Eliprodil 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Eliprodil 的部分引用包括：
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
Rennekamp et al (2016) σ1 receptor ligands control a switch between passive and active threat responses. Nat Chem Biol 12 552 PMID: 27239788
Eliprodil 的评论
平均评分: 5 (Based on 1 Review.)
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Evaluate the efficacity and the window of therapeutic opportunity of Eliprodil.
By
Anonymous on 12/17/2019
种属： Human
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.
该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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