threo Ifenprodil hemitartrate

threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity[1][2][3].

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

IC50: 0.22 μM (NMDA)[1].

[1]. Hashimoto K, et al. Interactions of erythro-ifenprodil, threo-ifenprodil, erythro-iodoifenprodil, and eliprodil with subtypes of sigma receptors. Eur J Pharmacol. 1995 Feb 6;273(3):307-10.  

[2]. Avenet P, et al. 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. 1996 Jan 25;296(2):209-13.  

[3]. Monassier L, et al. sigma(2)-receptor ligand-mediated inhibition of inwardly rectifying K(+) channels in the heart. J Pharmacol Exp Ther. 2007 Jul;322(1):341-50.