Memantine

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Chemical Structure| 19982-08-2 同义名 : 3,5-二甲基金刚烷-1-胺
CAS号 : 19982-08-2
货号 : A611376
分子式 : C12H21N
纯度 : 97%
分子量 : 179.3
MDL号 : MFCD02114015
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 9 mg/mL(50.19 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Memantine is a non-competitive N-methyl-d-aspartate receptor antagonist currently used for the treatment of Alzheimer's disease as an approved indication[3]. A therapeutic dose of memantine 10 mg/kg yielded more protection than 5 mg/kg in the treatment of neuropathy[4]. Treatment of animals with memantine (10 or 20 mg/kg) either before or after MDMA (10 mg/kg) administration significantly decreased the peak body temperature. The inhibitory effect of memantine on MDMA-induced hyperthermia may be due to its activity as an NMDA receptor antagonist and not as a result of a direct effect on the 5-HT or DA systems[5]. Pretreatment of memantine hydrochloride (10-30 mg/kg., i.p.) dose-dependently delayed the onset of different phases of convulsions induced by NMDA[6]. Memantine treatment can prevent okadaic acid induced impairment of hippocampal-dependent spatial memory and accompanied by modulation of the expression level of α7 subunit of nACh and NR2B subunit of NMDA receptors in the hippocampus[7]. 7-day intraperitoneal application of memantine, at doses of 5 mg/kg or 20 mg/kg, did not alter hippocampal long-term potentiation induction in rats, while 40 mg/kg memantine presented potent long-term potentiation inhibition. 20 mg/kg memantine attenuated the potent long-term potentiation inhibition caused by exposure to amyloid-β protein in the dentate gyrus in vitro. The antagonizing effect of long-term systematic treatment of memantine against amyloid-β protein triggered long-term potentiation inhibition to improve synaptic plasticity[8].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00630500 Dementia Associated With Parki... 展开 >>nson's Disease Dementia With Lewy Bodies 收起 << Phase 2 Completed - Norway ... 展开 >> Stavanger University Hospital, Old Age Psychiatry Clinic Stavanger, Norway, 4005 Sweden Clinical Memory Research Unit, Neuropsychiatric Clinic, University Hospital Malmo Malmo, Sweden, 20502 United Kingdom Mental Health Unit Epping, Essex, United Kingdom, CM16 6TN King's COllege London London, United Kingdom, SE1 1UL 收起 <<
NCT00148590 Schizophrenia Phase 3 Terminated - Germany ... 展开 >> Charité Universitaetsmedizin Berlin; Campus Charité Mitte; Dept. for Psychiatry and Psychotherapy Berlin, Germany, 10117 收起 <<
NCT03569579 Central Nervous System Disease... 展开 >>s 收起 << Phase 1 Completed - Korea, Republic of ... 展开 >> Chonbuk National University Hospital Jeonju, Korea, Republic of 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.58mL

1.12mL

0.56mL

27.89mL

5.58mL

2.79mL

55.77mL

11.15mL

5.58mL

参考文献

[1]Laube B, Hirai H, et al. Molecular determinants of agonist discrimination by NMDA receptor subunits: analysis of the glutamate binding site on the NR2B subunit. Neuron. 1997 Mar;18(3):493-503.

[2]Neumann S, Huang W, et al. A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. Endocrinology. 2010 Jul;151(7):3454-9.

[3]Lu S, Nasrallah HA. The use of memantine in neuropsychiatric disorders: An overview. Ann Clin Psychiatry. 2018 Aug;30(3):234-248

[4]Salih NA, Al-Baggou BK. Effect of memantine hydrochloride on cisplatin-induced neurobehavioral toxicity in mice. Acta Neurol Belg. 2020 Feb;120(1):71-82

[5]Nisijima K, Kuboshima K, Shioda K, Yoshino T, Iwamura T, Kato S. Memantine attenuates 3,4-methylenedioxymethamphetamine-induced hyperthermia in rats. Neurosci Lett. 2012 Dec 7;531(2):198-203

[6]Dhir A, Chopra K. Memantine delayed N-methyl-D-aspartate -induced convulsions in neonatal rats. Fundam Clin Pharmacol. 2015 Feb;29(1):72-8

[7]Dashniani MG, Chighladze MR, Solomonia RO, Burjanadze MA, Kandashvili M, Chkhikvishvili NC, Beselia GV, Kruashvili LB. Memantine treatment prevents okadaic acid induced neurotoxicity at the systemic and molecular levels. Neuroreport. 2020 Mar 4;31(4):281-286

[8]Li F, Chen X, Wang F, Xu S, Chang L, Anwyl R, Wang Q. Chronic pre-treatment with memantine prevents amyloid-beta protein-mediated long-term potentiation disruption. Neural Regen Res. 2013 Jan 5;8(1):49-55