Neramexane Explained
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, Alzheimer's disease,[4] drug addiction[5] and as an analgesic.[6] Animal studies have also suggested antidepressant[7] and nootropic[8] actions so that this drug may be used for a wide range of potential applications. It also acts as a nicotinic acetylcholine receptor antagonist.[9]
A clinical trial found that doses of 50 mg and above safely improved tinnitus scores over 16 weeks.[10]
See also
Notes and References
- 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 . 114 . 12 . 1529–37 . 2007 . 17728997 . 10.1007/s00702-007-0792-7 . 8654883 .
- 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 . 8 . 10 . 835–43 . 2002 . 11945134 . 10.2174/1381612024607117 .
- Danysz W, Parsons CG . Neuroprotective potential of ionotropic glutamate receptor antagonists . Neurotoxicity Research . 4 . 2 . 119–26 . March 2002 . 12829411 . 10.1080/10298420290015872 . 9413469 .
- Rammes G, Schierloh A . Neramexane (merz pharmaceuticals/forest laboratories) . IDrugs . 9 . 2 . 128–35 . February 2006 . 16523403 .
- Kotlinska J, Biala G, Rafalski P, Bochenski M, Danysz W . Effect of neramexane on ethanol dependence and reinforcement . European Journal of Pharmacology . 503 . 1–3 . 95–8 . October 2004 . 15496302 . 10.1016/j.ejphar.2004.09.036 .
- 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 . 12 . 1 . 17–29 . January 2008 . 17449306 . 10.1016/j.ejpain.2007.02.002 . 2875679 .
- 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 . The Journal of Pharmacology and Experimental Therapeutics . 318 . 3 . 1128–36 . September 2006 . 16740621 . 10.1124/jpet.106.103697 . 11450694 .
- 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 Behavior . 85 . 2 . 298–306 . October 2006 . 17045636 . 10.1016/j.pbb.2006.08.011 . 9614195 .
- Plazas PV, Savino J, Kracun S, Gomez-Casati ME, Katz E, Parsons CG, Millar NS, Elgoyhen AB . 6 . 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 . July 2007 . 17466293 . 10.1016/j.ejphar.2007.03.026 . 11336/79674 . free .
- Suckfüll M, Althaus M, Ellers-Lenz B, Gebauer A, Görtelmeyer R, Jastreboff PJ, Moebius HJ, Rosenberg T, Russ H, Wirth Y, Krueger H . 6 . 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 . January 2011 . 21223542 . 3031239 . 10.1186/1472-6815-11-1 . free .