threo Ifenprodil hemitartrateCat No. 2892 |
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Chemical Name: (1S*,2S*)-threo-2-(4-Benzylpiperidino)-1-(4-hydroxyphen yl)-1-propanol hemitartrate |
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Biological Activity
Potent σ receptor agonist (Ki values are 59.1 and 2 nM for σ1 and σ2 receptors respectively) and NR2B subunit-selective NMDA receptor antagonist (IC50 values are 0.22 and 324.8 μM at NR2B and NR2A 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.Technical Data
M.Wt:The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.
Resources
Certificate of Analysis / MSDS
References
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. 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. Monassier et al (2007) σ2-receptor ligand-mediated inhibition of inwardly rectifying K+ channels in the heart. J.Pharmacol.Exp.Ther. 322 341.If you know of a useful citation for this product please let us know.
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Keywords: threo Ifenprodil hemitartrate, NR2B, selective, NMDA, antagonists, receptors, s, σ, sigma, agonist, ionotropic, glutamate, iGluR
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