Amantadine
(Synonyms: 金刚烷胺; 1-Adamantanamine; 1-Aminoadamantane) 目录号 : GC63814
An NMDA receptor antagonist and antiviral agent
Cas No.:768-94-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amantadine is an NMDA receptor antagonist with IC50 values of 0.93, 0.82, and 0.47 μM at -70 mV for NR1-1a/NR2A, NR1-1a/NR2B, and NR1-1a/NR2D subunit-containing recombinant receptors, respectively, expressed in HEK293 cells.1 It blocks the influenza A M2 proton channel (IC50 = 16 μM for the recombinant channel expressed in Xenopus oocytes) and inhibits cytotoxicity induced by the influenza A strains H1N1 and H3N2 in MDCK cells (EC50s = 34 and 0.84 μM, respectively).2 It also improves the survival of mice infected with influenza A when administered 24 hours following viral challenge at a dose of 100 mg/kg per day.3 Amantadine (40 mg/kg) decreases dyskinesia induced by L-DOPA in a 6-OHDA hemi-parkinsonian mouse model.4 Formulations containing amantadine have been used in the treatment of various strains of influenza A virus infection and in the treatment of parkinsonism and drug-induced extrapyramidal symptoms.
1.Bresink, I., Benke, T.A., Collett, V.J., et al.Effects of memantine on recombinant rat NMDA receptors expressed in HEK 293 cellsBr. J. Pharmacol.119(2)195-204(1996) 2.Rey-Carrizo, M., Torres, E., Ma, C., et al.3-Azatetracyclo[5.2.1.15,8.01,5]undecane derivatives: From wild-type inhibitors of the M2 ion channel of influenza A virus to derivatives with potent activity against the V27A mutantJ. Med. Chem.56(22)9265-9274(2013) 3.Smee, D.F., Julander, J.G., Tarbet, E.B., et al.Treatment of oseltamivir-resistant influenza A (H1N1) virus infections in mice with antiviral agentsAntiviral Res.96(1)13-20(2012) 4.Bido, S., Marti, M., and Morari, M.Amantadine attenuates levodopa-induced dyskinesia in mice and rats preventing the accompanying rise in nigral GABA levelsJ. Neurochem.118(6)1043-1055(2011)
| Cas No. | 768-94-5 | SDF | Download SDF |
| 别名 | 金刚烷胺; 1-Adamantanamine; 1-Aminoadamantane | ||
| 分子式 | C10H17N | 分子量 | 151.25 |
| 溶解度 | DMSO : 1mg/mL | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.6116 mL | 33.0579 mL | 66.1157 mL |
| 5 mM | 1.3223 mL | 6.6116 mL | 13.2231 mL |
| 10 mM | 0.6612 mL | 3.3058 mL | 6.6116 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Amantadine and memantine: a comprehensive review for acquired brain injury
Brain Inj 2020 Feb 23;34(3):299-315.PMID:32078407DOI:10.1080/02699052.2020.1723697.
This comprehensive review discusses clinical studies of patients following brain injuries (traumatic, acquired, or stroke), who have been treated with Amantadine or memantine. Both Amantadine and memantine are commonly used in the acute rehabilitation setting following brain injuries, despite their lack of FDA-approval for neuro-recovery. Given the broad utilization of such agents, there is a need to review the evidence supporting this common off-label prescribing. The purpose of this review is to describe the mechanisms of action for memantine and Amantadine, as well as to complete a comprehensive review of the clinical uses of these agents. We included 119 original, clinical research articles from NCBI Medline, published before 2019. We focused on the domains of neuroplasticity, functional recovery, motor recovery, arousal, fatigue, insomnia, behavior, agitation, and cognition. Most of the existing research supporting the use of Amantadine and memantine in recovery from brain injuries was done in very small populations, limiting the significance of conclusions. While most studies are positive; small effect sizes are usually reported, or populations are subject to bias. Furthermore, evidence is so limited that this review includes research regarding both acute and chronic acquired brain injury populations. Fortunately, reported short-term side effects generally are modest, and stop soon after Amantadine/memantine is discontinued. However, responses are inconsistent, and the phenotype of responders remains elusive.
[Amantadine]
Nihon Rinsho 2003 Nov;61(11):1967-74.PMID:14619440doi
Amantadine is the first antiviral drug for human which was developed by duPont chemical company in 1964. Amantadine causes a selective, dose-related effectiveness of type A influenza virus and cost performance is very high. Amantadine should be given within 48 hours from onset of influenza. Daily doses should not exceed 150 mg in children, 200 mg in adults and less than 100 mg for renal insufficiency. The faulty point of Amantadine is that influenza virus becomes easily resistant to the drug through aminoacids change of ionchannel of M2 protein. Fortunately resistant virus is less virulent and has short life in practical meaning. As rapid diagnostic kits are conveniently available for influenza, you should choice Amantadine when the patient was positive for type A influenza by kit, especially neuraminidase inhibitor drugs became shortage.
Extended-Release Amantadine for Levodopa-Induced Dyskinesia
Expert Rev Neurother 2019 Apr;19(4):293-299.PMID:30892103DOI:10.1080/14737175.2019.1592677.
Levodopa-induced dyskinesia (LID) is a significant impediment to the long-term use of levodopa for Parkinson's disease (PD). Relatively few studies exist that have described safe and effective therapy for LID. There is thus a significant need for therapy that can control LID to allow for greater sustainability of levodopa therapy. Amantadine extended release (ER) is currently the only FDA-approved medication for the treatment of LID. While other medications have demonstrated efficacy in treating the motor symptoms of PD, Amantadine ER is the only one that has been shown, in several clinical trials, to reduce LID and reduce OFF time. Areas Covered: In this review, the authors present the findings of Amantadine ER including its efficacy and safety. The authors also provide their expert perspectives on its use and its future prospects. Expert opinion: Several therapies are currently being used and studied for controlling LID, an unmet need in therapy for PD. Amantadine ER has potential to supplement levodopa therapy in PD and improve patient therapeutic outcomes.
[Amantadine-induced livedo reticularis]
Hautarzt 1998 Mar;49(3):224-7.PMID:9565792DOI:10.1007/s001050050732.
A 63-year old women developed livedo reticularis during treatment with Amantadine. This reversible side effect of Amantadine has been most often seen in women and is frequently associated with persistent ankle edema. We discuss the signs and symptoms, pathogenesis and treatment of amantadine-induced livedo reticularis.
[Anti-inflammatory effects of Amantadine and memantine in SARS-CoV-2 infection]
Pol Merkur Lekarski 2021 Feb 24;49(289):67-70.PMID:33713098doi
Amantadine and memantine, apart from their action on cholinergic receptors and dopamine secretion, have a significant influence on the inflammatory process, including the so-called "cytokine storm" and reduction of apoptosis and oxidative stress. Amantadine also inhibits the induction of inflammatory factors such as RANTES, activates kinase p38 of mitogen-activated protein (MAP) and c-Jun-NH2-terminal kinases (JNK), which inhibit viral replication. It also significantly inhibits the entry of SARS-CoV-2 into the bronchial epithelial cell and blocks the viroporin proton channel of the virus. In addition, it has the ability to pass through the membrane of lysosomes into their interior and act as an alkalizing agent, which prevents the release of viral RNA into the cell, which may be a key element in therapeutic management. Memantine also reduces inflammation, mainly in the nervous system, but also acts as a lysosomotropic factor, inhibiting viral replication. However, it is important to bear in mind when undertaking Amantadine or memantine therapy with side effects that may overlap with COVID- 19 symptoms, worsening the condition of patients. Currently, the effectiveness of Amantadine and memantine in the treatment of patients with COVID-19 symptoms has been demonstrated in a few clinical trials, mainly in patients treated for neurodegenerative diseases. The obtained results are of considerable value, but require confirmation in further studies.