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 that this drug may be used for a wide range of potential applications. It also acts as a nicotinic acetylcholine receptor antagonist.^[11]

ATC code

none

CAS Number

219810-59-0^Y

PubChem CID

6433106

ChemSpider

4938294^N

Quick facts Clinical data, ATC code ...

Neramexane
Clinical data

ATC code	none
Identifiers
IUPAC name 1,3,3,5,5-pentamethylcyclohexanamine
CAS Number	219810-59-0^Y
PubChem CID	6433106
ChemSpider	4938294^N
UNII	856DX0KJ84
CompTox Dashboard (EPA)	DTXSID40176399
ECHA InfoCard	100.107.752
Chemical and physical data
Formula	C₁₁H₂₃N
Molar mass	169.312 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C1(C)(N)CC(C)(C)CC(C)(C)C1
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]

[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. hdl:11336/79674. 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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