threo Ifenprodil hemitartrate

Biological Activity

threo Ifenprodil hemitartrate is a potent σ receptor agonist (K_i 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.

Technical Data

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.

Background References

1. Rapid synaptic potentiation within the anterior cingulate cortex mediates trace fear learning.
   
   Mol Brain, 2012;5(0):6.
2. Interactions of erythro-ifenprodil, threo-ifenprodil and erythro-iodoifenprodil, and eliprodil with subtypes of σ receptors.
   Hashimoto and London
   Eur.J.Pharmacol., 1995;273:307
3. Antagonist properties of the stereoisomers of ifenprodil at NR1A/NR2A and NR1A/NR2B subtypes of the NMDA receptor expressed in Xenopus oocytes.
   Avenet et al.
   Eur.J.Pharmacol., 1996;296:209
4. σ₂-receptor ligand-mediated inhibition of inwardly rectifying K⁺channels in the heart.
   Monassier et al.
   J.Pharmacol.Exp.Ther., 2007;322:341

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