Neramexane

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]

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
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
 NY (what is this?)  (verify)

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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