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MedKoo Cat#: 414333 | Name: Neramexane Free Base

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Neramexane Free Base is a drug related to memantine, which acts as an NMDA antagonist and has neuroprotective effects. It is being developed for various possible applications, including treatment of tinnitus, Alzheimer's disease, drug addiction and as an analgesic.

Chemical Structure

Neramexane Free Base
Neramexane Free Base
CAS#219810-59-0 (free base)

Theoretical Analysis

MedKoo Cat#: 414333

Name: Neramexane Free Base

CAS#: 219810-59-0 (free base)

Chemical Formula: C11H23N

Exact Mass: 169.1830

Molecular Weight: 169.31

Elemental Analysis: C, 78.03; H, 13.69; N, 8.27

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Related CAS #
219810-59-0 (free base) 457068-92-7 (mesylate).
Synonym
Neramexane Free Base; MRZ2-579; MRZ-2-579; MRZ 2-579
IUPAC/Chemical Name
Cyclohexanamine, 1,3,3,5,5-pentamethyl-
InChi Key
OGZQTTHDGQBLBT-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H23N/c1-9(2)6-10(3,4)8-11(5,12)7-9/h6-8,12H2,1-5H3
SMILES Code
NC1(C)CC(C)(C)CC(C)(C)C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Neramexane Free Base is a drug related to memantine, which acts as an NMDA antagonist.
In vitro activity:
This study reports the effects of neramexane, a novel amino-alkyl-cyclohexane derivative that is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, on recombinant rat alpha9alpha10 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. The results indicate that both compounds block acetylcholine-evoked responses at micromolar concentrations with a rank order of potency of neramexane>memantine, P<0.05. Block by neramexane of acetylcholine responses was not overcome at high concentrations of the agonist, indicative of a non-competitive inhibition. Reference: Eur J Pharmacol. 2007 Jul 2;566(1-3):11-9. https://pubmed.ncbi.nlm.nih.gov/17466293/
In vivo activity:
Here this study determined the antinociceptive effect of chronic administration of neramexane and compared its effect with that of memantine and gabapentin in a rat model of diabetic neuropathic pain. Compared with vehicle-treated rats, treatment with neramexane (12.3, 24.6, and 49.2 mg/kg/day) for 2 weeks via an osmotic minipump produced dose-dependent and sustained effects on mechanical hyperalgesia and allodynia. Reference: Neuropharmacology. 2009 Aug;57(2):121-6. https://pubmed.ncbi.nlm.nih.gov/19422840/

Preparing Stock Solutions

The following data is based on the product molecular weight 169.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Plazas PV, Savino J, Kracun S, Gomez-Casati ME, Katz E, Parsons CG, Millar NS, Elgoyhen AB. Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptors. Eur J Pharmacol. 2007 Jul 2;566(1-3):11-9. doi: 10.1016/j.ejphar.2007.03.026. Epub 2007 Mar 24. PMID: 17466293. 2. Chen SR, Samoriski G, Pan HL. Antinociceptive effects of chronic administration of uncompetitive NMDA receptor antagonists in a rat model of diabetic neuropathic pain. Neuropharmacology. 2009 Aug;57(2):121-6. Doi: 10.1016/j.neuropharm.2009.04.010. Epub 2009 May 5. PMID: 19422840; PMCID: PMC2743295. 3. 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. J Pharmacol Exp Ther. 2006 Sep;318(3):1128-36. doi: 10.1124/jpet.106.103697. Epub 2006 Jun 1. PMID: 16740621.
In vitro protocol:
1. Plazas PV, Savino J, Kracun S, Gomez-Casati ME, Katz E, Parsons CG, Millar NS, Elgoyhen AB. Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptors. Eur J Pharmacol. 2007 Jul 2;566(1-3):11-9. doi: 10.1016/j.ejphar.2007.03.026. Epub 2007 Mar 24. PMID: 17466293.
In vivo protocol:
1. Chen SR, Samoriski G, Pan HL. Antinociceptive effects of chronic administration of uncompetitive NMDA receptor antagonists in a rat model of diabetic neuropathic pain. Neuropharmacology. 2009 Aug;57(2):121-6. Doi: 10.1016/j.neuropharm.2009.04.010. Epub 2009 May 5. PMID: 19422840; PMCID: PMC2743295. 2. 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. J Pharmacol Exp Ther. 2006 Sep;318(3):1128-36. doi: 10.1124/jpet.106.103697. Epub 2006 Jun 1. PMID: 16740621.
1: Suckfüll M, Althaus M, Ellers-Lenz B, Gebauer A, Görtelmeyer R, Jastreboff PJ, Moebius HJ, Rosenberg T, Russ H, Wirth Y, Krueger H. 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 Throat Disord. 2011 Jan 11;11:1. doi: 10.1186/1472-6815-11-1. PubMed PMID: 21223542; PubMed Central PMCID: PMC3031239. 2: Rammes G. Neramexane: a moderate-affinity NMDA receptor channel blocker: new prospects and indications. Expert Rev Clin Pharmacol. 2009 May;2(3):231-8. doi: 10.1586/ecp.09.7. PubMed PMID: 24410702. 3: Plazas PV, Savino J, Kracun S, Gomez-Casati ME, Katz E, Parsons CG, Millar NS, Elgoyhen AB. Inhibition of the alpha9alpha10 nicotinic cholinergic receptor by neramexane, an open channel blocker of N-methyl-D-aspartate receptors. Eur J Pharmacol. 2007 Jul 2;566(1-3):11-9. Epub 2007 Mar 24. PubMed PMID: 17466293. 4: 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. Eur J Pain. 2008 Jan;12(1):17-29. Epub 2007 Apr 20. PubMed PMID: 17449306. 5: 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. Pharmacol Biochem Behav. 2006 Oct;85(2):298-306. Epub 2006 Oct 11. PubMed PMID: 17045636. 6: 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. J Pharmacol Exp Ther. 2006 Sep;318(3):1128-36. Epub 2006 Jun 1. PubMed PMID: 16740621. 7: Rammes G, Schierloh A. Neramexane (merz pharmaceuticals/forest laboratories). IDrugs. 2006 Feb;9(2):128-35. Review. PubMed PMID: 16523403. 8: Bachteler D, Economidou D, Danysz W, Ciccocioppo R, Spanagel R. The effects of acamprosate and neramexane on cue-induced reinstatement of ethanol-seeking behavior in rat. Neuropsychopharmacology. 2005 Jun;30(6):1104-10. PubMed PMID: 15668725. 9: Kotlinska J, Biala G, Rafalski P, Bochenski M, Danysz W. Effect of neramexane on ethanol dependence and reinforcement. Eur J Pharmacol. 2004 Oct 25;503(1-3):95-8. PubMed PMID: 15496302. 10: Sukhotina IA, Zvartau EE, Danysz W, Bespalov AY. Caffeine withdrawal syndrome in social interaction test in mice: effects of the NMDA receptor channel blockers, memantine and neramexane. Behav Pharmacol. 2004 May;15(3):207-14. PubMed PMID: 15187578. 11: Neramexane. Drugs R D. 2002;3(1):19-20. Review. PubMed PMID: 11881523.