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Submit Reviewthreo Ifenprodil hemitartrate
说明： GluN2B-selective NMDA antagonist; also σ agonist
化学名： (1S*,2S*)-threo-2-(4-Benzylpiperidino)-1-(4-hydroxyphenyl)-1-propanol hemitartrate
纯度： ≥98% (HPLC)
生物活性 for threo Ifenprodil hemitartrate
threo Ifenprodil hemitartrate is a potent σ receptor agonist (Ki values are 59.1 and 2 nM for σ1 and σ2 receptors respectively) and GluN2B (formally NR2B) subunit-selective NMDA receptor antagonist (IC50 values are 0.22 and 324.8 μM at GluN2B and GluN2A respectively). Displays ~8-fold reduced affinity at α-adrenoceptors compared to Ifenprodil (Cat.No. 0545). Inhibits the hERG potassium channel (IC50 = 88 nM) and exhibits antiarrhythmic activity in vivo.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
技术数据 for threo Ifenprodil hemitartrate
| 分子量 | 400.49 |
| 公式 | C21H27NO2.½C4H6O6 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| PubChem ID | 11957579 |
| InChI Key | DMPRDSPPYMZQBT-UHFFFAOYSA-N |
| Smiles | OC(C=C3)=CC=C3[C@H](O)[C@H](C)N2CCC(CC2)CC1=CC=CC=C1.OC(C=C6)=CC=C6[C@H](O)[C@H](C)N5CCC(CC5)CC4=CC=CC=C4.OC(C=C9)=CC=C9[C@@H](O)[C@@H](C)N8CCC(CC8)CC7=CC=CC=C7.OC(C=C%12)=CC=C%12[C@@H](O)[C@@H](C)N%11CCC(CC%11)CC%10=CC=CC=C%10.O=C(O)C(O)C(O)C(O)=O.O=C(O)C(O)C(O)C(O)=O |
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 threo Ifenprodil hemitartrate
参考文献 for threo Ifenprodil hemitartrate
参考文献是支持产品生物活性的出版物。
Hashimoto and London (1995) Interactions of erythro-ifenprodil, threo-ifenprodil and erythro-iodoifenprodil, and eliprodil with subtypes of σ receptors. Eur.J.Pharmacol. 273 307 PMID: 7737340
Avenet et al (1996) Antagonist properties of the stereoisomers of ifenprodil at NR1A/NR2A and NR1A/NR2B subtypes of the NMDA receptor expressed in Xenopus oocytes. Eur.J.Pharmacol. 296 209 PMID: 8838458
Monassier et al (2007) σ2-receptor ligand-mediated inhibition of inwardly rectifying K+channels in the heart. J.Pharmacol.Exp.Ther. 322 341 PMID: 17460149
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关键词: threo Ifenprodil hemitartrate, threo Ifenprodil hemitartrate supplier, NR2B, selective, NMDA, antagonists, receptors, s, σ, sigma, agonist, ionotropic, glutamate, iGluR, GluN2B, Sigma-Related, Receptors, 2892, Tocris Bioscience
2 篇 threo Ifenprodil hemitartrate 的引用文献
引用文献是使用了 Tocris 产品的出版物。 threo Ifenprodil hemitartrate 的部分引用包括：
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
Gasperini et al (2015) Prion protein and copper cooperatively protect neurons by modulating NMDA receptor through S-nitrosylation. Sci Rep 22 772 PMID: 25490055
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