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Memantine hydrochloride is an antagonist at the NMDA receptor (IC50 = 0.5 -1.5 μM in vitro), binding to the ion channel site. Memantine increases BDNF protein and mRNA levels in the brain in vivo. In an animal model of Alzheimer's disease, memantine improves spatial learning and decreases deposition of Aβ plaques. Memantine has neuroprotective effects in dopaminergic neurons; stimulates release of neurotrophic factor from astroglia and reduces microglia inflammation in vitro.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 215.77. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.63 mL||23.17 mL||46.35 mL|
|5 mM||0.93 mL||4.63 mL||9.27 mL|
|10 mM||0.46 mL||2.32 mL||4.63 mL|
|50 mM||0.09 mL||0.46 mL||0.93 mL|
References are publications that support the biological activity of the product.
Chen et al (1998) Neuroprotective concentrations of the N-MthD.-aspartate open-channel blocker Mem. are effective without cytoplasmic vacuolation following post-ischemic administration and do not block maze learning or long-term potentiation. Neuroscience 86 1121 PMID: 9697119
Parsons et al (1999) Mem. is a clinically well tolerated N-MthD.-aspartate (NMDA) receptor antagonist - a review of preclinical data. Neuropharmacology 38 735 PMID: 10465680
Parsons et al (2007) Mem.: A NMDA receptor antagonist that improves memory by restoration of homeostasis in the glutamatergic system - too little activation is bad, too much is even worse. Neuropharmacology 53 699 PMID: 17904591
Zajaczkowski et al (1997) Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP. Neuropharmacology 36 961 PMID: 9257940
Wu et al (2009) Novel neuroprotective mechanisms of memantine: increase in neurotrophic factor release from astroglia and anti-inflammation by preventing microglial activation. Neuropsychopharmacology 34 2344 PMID: 19536110
Dong et al (2008) Effects of memantine on neuronal structure and conditioned fear in the Tg2576 mouse model of Alzheimer's disease. Neuropsychopharmacology 33 3226 PMID: 18418360
Minkeviciene et al (2004) Memantine improves spatial learning in a transgenic mouse model of Alzheimer's disease. J.Pharmacol.Exp.Ther. 311 677 PMID: 15192085
If you know of a relevant reference for Memantine hydrochloride, please let us know.
Keywords: Memantine hydrochloride, Memantine hydrochloride supplier, NMDA, antagonists, ion, channel, site, glutamate, receptors, N-Methyl-D-Aspartate, iGluR, ionotropic, BDNFparkinsons, alzheimers, neurodegeneration, neurodegenerative, disease, Receptors, 0773, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Memantine hydrochloride include:
He and Bausch (2014) Synaptic plasticity in glutamatergic and GABAergic neurotransmission following chronic Mem. treatment in an in vitro model of limbic epileptogenesis. J Neurosci 77 379 PMID: 24184417
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
Jaekel et al (2006) Neuroprotection associated with alternative splicing of NMDA receptors in rat cortical neurons. Neuropharmacology 147 622 PMID: 16314856
Sachser et al (2016) Forgetting of long-term memory requires activation of NMDA receptors, L-type voltage-dependent Ca(2+) channels, and calcineurin. Sci Rep 6 22771 PMID: 26947131
Birnbaum et al (2015) Calcium flux-independent NMDA receptor activity is required for Aβ oligomer-induced synaptic loss. J Neurosci 6 e1791 PMID: 26086964
Campbell et al (2015) Functional changes in glutamate transporters and astrocyte biophysical properties in a rodent model of focal cortical dysplasia. Invest Ophthalmol Vis Sci 8 425 PMID: 25565960
Carlson et al (2012) Pharmacological evidence that D-aspartate activates a current distinct from ionotropic glutamate receptor currents in Aplysia californica. Brain Behav 2 391 PMID: 22950043
Fan and Cooper (2009) Glutamate-induced NFκB activation in the retina. Proc Natl Acad Sci U S A 50 917 PMID: 18836176
Rzeski et al (2001) Glutamate antagonists limit tumor growth. FASEB J 98 6372 PMID: 11331750
Bali et al (2019) Cognitive enhancer effects of low Mem. doses are facilitated by an alpha7 nicotinic acetylcholine receptor agonist in scopolamine-induced amnesia in rats. Front Pharmacol 10 73 PMID: 30804787
Simma et al (2014) NMDA-receptor antagonists block B-cell function but foster IL-10 production in BCR/CD40-activated B cells. Front Cell Neurosci 12 75 PMID: 25477292
Puddifoot et al (2009) Pharmacological characterization of recombinant NR1/NR2A NMDA receptors with truncated and deleted carboxy termini expressed in Xenopus laevis oocytes. Br J Pharmacol 156 509 PMID: 19154422
Bouchard-Cannon et al (2018) Dexras1 is a homeostatic regulator of exercise-dependent proliferation and cell survival in the hippocampal neurogenic niche. Sci Rep 8 5294 PMID: 29593295
Manning et al (2008) NMDA receptor blockade with Mem. attenuates white matter injury in a rat model of periventricular leukomalacia. Cell Commun Signal 28 6670 PMID: 18579741
Léveillé et al (2008) Neuronal viability is controlled by a functional relation between synaptic and extrasynaptic NMDA receptors. FASEB J 22 4258 PMID: 18711223
Costa et al (2008) Electrophysiology and pharmacology of striatal neuronal dysfunction induced by mitochondrial complex I inhibition. J Neurosci 28 8040 PMID: 18685029
Kaufman et al (2012) Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons. Cell Death Dis 32 3992 PMID: 22442066
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Memantine was used as a use-dependent blocker of NMDA receptors in nucleated patches pulled from stem-cell-derived dopamine neurons. Application of 0.5 µM memantine induced a significant decrease of NMDA receptors response. Washout for 4-5 minutes commonly returned the response amplitude to control values (see illustration).
We have been using memantine hydrochloride from Tocris for behavioral pharmacology and in vivo electrophysiology in rats. In electrophysiology experiments, memantine was delivered with microiontophoresis into the close vicinity of the neurons during recording in the rat cerebral cortex. Memantine was successfully applied from glass micropipettes of multi-barrel electrodes with positive constant currents at acidic pH, and it exerted the expected effect on hippocampal neurons (see attached figure of a representative recording).In behavioral experiments, memantine enhanced cognitive function in scopolamine-induced transient amnesia in rats. However, we found that memantine was effective at substantially lower doses compared to most of the publications from other laboratories.
It is recommended to always perform an initial experiment for the assessment of the dose-response curve, and not to rely on available literature data regarding suggested suitable doses, since the effect of memantine may substantially differ in different assays or behavioral paradigms.
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