Therapeutics

Neramexane

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Overview

Name: Neramexane
Synonyms: MRZ 2/579
Chemical Name: 1,3,3,5,5-pentamethylcyclohexanamine
Therapy Type: Small Molecule (timeline)
Target Type: Other Neurotransmitters (timeline)
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Discontinued)
Company: Forest Laboratories, Inc., Merck
Approved for: None

Background

Similar to memantine, neramexane is an NMDA receptor channel blocker with moderate affinity. It displays voltage dependency, and rapid unblocking kinetics (Gilling et al., 2007). Neramexane also has been shown to block acetylcholine-evoked responses by antagonizing the alpha-9 alpha-10 nicotinic acetylcholine receptor (Plazas et al., 2007).

Last Updated: 12 Dec 2013

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References

Paper Citations

  1. Gilling K, Jatzke C, Wollenburg C, Vanejevs M, Kauss V, Jirgensons A, Parsons CG. A novel class of amino-alkylcyclohexanes as uncompetitive, fast, voltage-dependent, N-methyl-D-aspartate (NMDA) receptor antagonists--in vitro characterization. J Neural Transm. 2007;114(12):1529-37. Epub 2007 Aug 31 PubMed.
  2. Plazas PV, Savino J, Kracun S, Gomez-Casati ME, Katz E, Parsons CG, Millar NS, Elgoyhen AB. Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptors. Eur J Pharmacol. 2007 Jul 2;566(1-3):11-9. PubMed.

Further Reading

No Available Further Reading