1312991-83-5
1312991-83-5
Chemical Structure
threo-Ifenprodil hemitartrate
- CAS No.: 1312991-83-5
- Formula:C21H27NO2.1/2C4H6O6
- Molecular Weight:400.50
SMILES: OC([C@H](O)[C@@H](O)C(O)=O)=O.O[C@H](C1=CC=C(C=C1)O)[C@@H](C)N(CC2)CCC2CC3=CC=CC=C3.[1/2]
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
