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Submit ReviewMemantine hydrochloride
说明： NMDA antagonist; acts at ion channel site
化学名： 3,5-Dimethyl-tricyclo[3.3.1.13,7]decan-1-amine hydrochloride
生物活性 for Memantine hydrochloride
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.
技术数据 for Memantine hydrochloride
| 分子量 | 215.77 |
| 公式 | C12H21N.HCl |
| 储存 | Store at RT |
| CAS Number | 41100-52-1 |
| PubChem ID | 181458 |
| InChI Key | LDDHMLJTFXJGPI-UHFFFAOYSA-N |
| Smiles | NC12CC3(CC(C1)(CC(C2)C3)C)C.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Memantine hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 100 |
制备储备液 for Memantine hydrochloride
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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 |
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产品说明书 for Memantine hydrochloride
参考文献 for Memantine hydrochloride
参考文献是支持产品生物活性的出版物。
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.
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关键词: 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
17 篇 Memantine hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Memantine hydrochloride 的部分引用包括：
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
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
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
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
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
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
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
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
Rzeski et al (2001) Glutamate antagonists limit tumor growth. FASEB J 98 6372 PMID: 11331750
Jaekel et al (2006) Neuroprotection associated with alternative splicing of NMDA receptors in rat cortical neurons. Neuropharmacology 147 622 PMID: 16314856
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Use-dependent block of NMDA receptors.
By
Sergiy Sylantyev on 10/15/2020
种属： Human
细胞系/组织： Stem cell - derived neurons
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).
Memantine hydrochloride in in vivo electrophysiology and in behavioral pharmacology.
By
Zsolt Bali on 03/01/2019
分析类型： In Vivo
种属： Rat
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.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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- Nuclear-Cytoplasmic Transport Interference
- Excitotoxicity
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