Neramexane

Neramexane
Clinical data
ATC code
  • none
Identifiers
IUPAC name
  • 1,3,3,5,5-pentamethylcyclohexanamine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
ECHA InfoCard100.107.752
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Chemical and physical data
FormulaC11H23N
Molar mass169.312 g·mol−1
3D model (JSmol)
SMILES
  • CC1(CC(CC(C1)(C)N)(C)C)C
InChI
  • InChI=1S/C11H23N/c1-9(2)6-10(3,4)8-11(5,12)7-9/h6-8,12H2,1-5H3 ☒N
  • Key:OGZQTTHDGQBLBT-UHFFFAOYSA-N ☒N
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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 50 mg and above safely improved tinnitus scores over 16 weeks.[12]

See also

References

  1. ↑ Gilling K, Jatzke C, Wollenburg C, Vanejevs M, Kauss V, Jirgensons A, Parsons CG (2007). "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. 114 (12): 1529–37. doi:10.1007/s00702-007-0792-7. PMID 17728997. S2CID 8654883.
  2. ↑ Danysz W, Parsons CG, Jirgensons A, Kauss V, Tillner J (2002). "Amino-alkyl-cyclohexanes as a novel class of uncompetitive NMDA receptor antagonists". Current Pharmaceutical Design. 8 (10): 835–43. doi:10.2174/1381612024607117. PMID 11945134.
  3. ↑ Danysz W, Parsons CG (March 2002). "Neuroprotective potential of ionotropic glutamate receptor antagonists". Neurotoxicity Research. 4 (2): 119–26. doi:10.1080/10298420290015872. PMID 12829411. S2CID 9413469.
  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 (February 2006). "Neramexane (merz pharmaceuticals/forest laboratories)". IDrugs. 9 (2): 128–35. PMID 16523403.
  7. ↑ Kotlinska J, Biala G, Rafalski P, Bochenski M, Danysz W (October 2004). "Effect of neramexane on ethanol dependence and reinforcement". European Journal of Pharmacology. 503 (1–3): 95–8. doi:10.1016/j.ejphar.2004.09.036. PMID 15496302.
  8. ↑ Klein T, Magerl W, Hanschmann A, Althaus M, Treede RD (January 2008). "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. 12 (1): 17–29. doi:10.1016/j.ejpain.2007.02.002. PMID 17449306. S2CID 2875679.
  9. ↑ Kos T, Legutko B, Danysz W, Samoriski G, Popik P (September 2006). "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". The Journal of Pharmacology and Experimental Therapeutics. 318 (3): 1128–36. doi:10.1124/jpet.106.103697. PMID 16740621. S2CID 11450694.
  10. ↑ Zoladz PR, Campbell AM, Park CR, Schaefer D, Danysz W, Diamond DM (October 2006). "Enhancement of long-term spatial memory in adult rats by the noncompetitive NMDA receptor antagonists, memantine and neramexane". Pharmacology, Biochemistry, and Behavior. 85 (2): 298–306. doi:10.1016/j.pbb.2006.08.011. PMID 17045636. S2CID 9614195.
  11. ↑ Plazas PV, Savino J, Kracun S, Gomez-Casati ME, Katz E, Parsons CG, et al. (July 2007). "Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptors". European Journal of Pharmacology. 566 (1–3): 11–9. doi:10.1016/j.ejphar.2007.03.026. PMID 17466293.
  12. ↑ Suckfüll M, Althaus M, Ellers-Lenz B, Gebauer A, Görtelmeyer R, Jastreboff PJ, et al. (January 2011). "A randomized, double-blind, placebo-controlled clinical trial to evaluate the efficacy and safety of neramexane in patients with moderate to severe subjective tinnitus". BMC Ear, Nose and Throat Disorders. 11: 1. doi:10.1186/1472-6815-11-1. PMC 3031239. PMID 21223542.


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