Neramexane

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Neramexane
Neramexane.svg
Systematic (IUPAC) name
1,3,3,5,5-pentamethylcyclohexanamine
Clinical data
Identifiers
219810-59-0 YesY
None
PubChem CID 6433106
ChemSpider 4938294 N
UNII 856DX0KJ84 YesY
Chemical data
Formula C11H23N
169.307 g/mol
 N (what is this?)  (verify)

Neramexane is a drug related to memantine,[1] which acts as an NMDA antagonist[2] and has neuroprotective effects.[3] It is being developed for various possible applications, including treatment of tinnitus,[4][5] Alzheimer's disease,[6] drug addiction[7] and as an analgesic.[8] Animal studies have also suggested antidepressant[9] and nootropic[10] actions, so there are a wide range of potential applications this drug may be used for. It also acts as a nicotinic acetylcholine receptor antagonist.[11]

A clinical trial found that doses of 50mg and above safely improved tinnitus scores over 16 weeks.[12]

See also[edit]

References[edit]

  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. Journal of Neural Transmission. 2007;114(12):1529-37. PMID 17728997
  2. ^ Danysz W, Parsons CG, Jirgensons A, Kauss V, Tillner J. Amino-alkyl-cyclohexanes as a novel class of uncompetitive NMDA receptor antagonists. Current Pharmaceutical Design. 2002;8(10):835-43. PMID 11945134
  3. ^ Danysz W, Parsons CG. Neuroprotective potential of ionotropic glutamate receptor antagonists. Neurotoxicity Research. 2002 Mar;4(2):119-26. PMID 12829411
  4. ^ Clinical trial number NCT00405886 for "Neramexane for Tinnitus" at ClinicalTrials.gov
  5. ^ Clinical trial number NCT00739635 for "Efficacy, Safety and Tolerability of Neramexane in Patients With Subjective Tinnitus" at ClinicalTrials.gov
  6. ^ Rammes G, Schierloh A. Neramexane (merz pharmaceuticals/forest laboratories). IDrugs. 2006 Feb;9(2):128-35. PMID 16523403
  7. ^ Kotlinska J, Biala G, Rafalski P, Bochenski M, Danysz W. Effect of neramexane on ethanol dependence and reinforcement. European Journal of Pharmacology. 2004 Oct 25;503(1-3):95-8. PMID 15496302
  8. ^ Klein T, Magerl W, Hanschmann A, Althaus M, Treede RD. Antihyperalgesic and analgesic properties of the N-methyl-D-aspartate (NMDA) receptor antagonist neramexane in a human surrogate model of neurogenic hyperalgesia. European Journal of Pain. 2008 Jan;12(1):17-29. PMID 17449306
  9. ^ Kos T, Legutko B, Danysz W, Samoriski G, Popik P. Enhancement of antidepressant-like effects but not brain-derived neurotrophic factor mRNA expression by the novel N-methyl-D-aspartate receptor antagonist neramexane in mice. Journal of Pharmacology and Experimental Therapeutics. 2006 Sep;318(3):1128-36. PMID 16740621
  10. ^ Zoladz PR, Campbell AM, Park CR, Schaefer D, Danysz W, Diamond DM. Enhancement of long-term spatial memory in adult rats by the noncompetitive NMDA receptor antagonists, memantine and neramexane. Pharmacology, Biochemistry and Behaviour. 2006 Oct;85(2):298-306. Epub 2006 Oct 11. PMID 17045636
  11. ^ Plazas PV, Savino J, Kracun S et al. (July 2007). "Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptors" 566 (1-3). pp. 11–9. doi:10.1016/j.ejphar.2007.03.026. 
  12. ^ "A randomized, double-blind, placebo-controlled clinical trial to evaluate the efficacy and safety of neramexane in patients with moderate to severe subjective tinnitus.". Jan 2011. PMID 21223542.