Galanthamine
(Synonyms: 加兰他敏; Galantamine) 目录号 : GC16573
An alkaloid with AChE inhibitory and nAChR potentiating activities
Cas No.:357-70-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1-3]: | |
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Cell lines |
Post-mortem human brain frontal cortex and hippocampus region, M10 cells, Rat pheochromocytoma (PC12) cells |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.35 μM |
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Applications |
Galanthamine inhibited the activity of acetylcholinesterase with the IC50 of 14 nM and 15 nM on AChE in post-mortem human brain frontal cortex and the hippocampus region. Red-cell cholinesterase activity in blood samples from the neurosurgery patients was 10 times more strongly inhibited by Galanthamine in brain tissue samples. Galanthamine (1 μM) activated single channels in outside-out patches excised from dexamethasone mouse fibroblasts (M10 cells). Galanthamine acts as noncompetitive nicotinic receptor agonists' on clonal rat pheochromocytoma (PC12) cells. Galanthamine (50 μM) activated single-channel currents in outside-out patches excised from clonal PC12 cells. |
| Animal experiment [4]: | |
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Animal models |
Male ddY mice |
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Dosage form |
Intraperitoneal injection, 0.3-3 mg/kg |
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Application |
Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increased IGF2 mRNA levels in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) increased fibroblast growth factor 2 mRNA levels and decreased brain-derived neurotrophic factor mRNA levels in the hippocampus. Galantamine increased hippocampal IGF2 protein. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Thomsen T, Kaden B, Fischer J P, et al. Inhibition of acetylcholinesterase activity in human brain tissue and erythrocytes by galanthamine, physostigmine and tacrine[J]. Clinical Chemistry and Laboratory Medicine, 1991, 29(8): 487-492. [2]. Pereira E F, Alkondon M, Reinhardt S, et al. Physostigmine and galanthamine: probes for a novel binding site on the alpha 4 beta 2 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells[J]. Journal of Pharmacology and Experimental Therapeutics, 1994, 270(2): 768-778. [3]. Storch A, Schrattenholz A, Cooper J C, et al. Physostigmine, galanthamine and codeine act as ‘noncompetitive nicotinic receptor agonists’ on clonal rat pheochromocytoma cells[J]. European Journal of Pharmacology: Molecular Pharmacology, 1995, 290(3): 207-219. [4]. Kita Y, Ago Y, Takano E, et al. Galantamine increases hippocampal insulin-like growth factor 2 expression via α7 nicotinic acetylcholine receptors in mice[J]. Psychopharmacology, 2013, 225(3): 543-551. | |
Galantamine is a potent inhibitor of acetylcholinesterase (AChE) with IC50 value of 410 nM. [1]
Acetylcholinesterase is a hydrolase. It belongs to carboxylesterase family of enzymes It hydrolyzes the neurotransmitter acetylcholine and has very high catalytic activity. AChE exits in many types of conducting tissue: nerve and muscle, motor and sensory fibers and central and peripheral tissues. AChE located on the post-synaptic membrane. It stops the signal transmission by hydrolyzing ACh. Ach plays an important role in neurotransmission. ACh is released into the synaptic cleft then binds to ACh receptors which located on the post-synaptic membrane. Inhibition the activity of AChE will result in impeded neurotransmission by leading to accumulation of ACh in the synaptic cleft. AChE also is an important target for Alzheimer disease.[1]
Galantamine significantly decreased apoptotic effect induced by thapsigargin at 300 nM in SH-SY5Y cells. Galantamine can more significantly increase cell viability in LDH assays at 10 nM in neuroblastoma cells. Galantamine at 300 nM increase the cell viability treated with Aβ. Galantamine significantly increaseed the expression level of Bcl-2 by 3.1 fold at 300nM in chromaffin cells.[1]
Galantamine can significantly incrase the mRNAs level of IGF2 at 3mg/kg in the mice hippoc ampus. Galantamine also transient decrease the BDNF mRNA levels and increase the FGF2 mRNA levels. Galantamine significantly increased the expression of IGF2 protein levels at 3 mg/kg in the hippocampus of mice.[2]
References:
[1]. Arias E, Ales E, Gabilan NH, Cano-Abad MF, Villarroya M, Garcia AG, Lopez MG: Galantamine prevents apoptosis induced by beta-amyloid and thapsigargin: involvement of nicotinic acetylcholine receptors. Neuropharmacology 2004, 46(1):103-114.
[2]. Kita Y, Ago Y, Takano E, Fukada A, Takuma K, Matsuda T: Galantamine increases hippocampal insulin-like growth factor 2 expression via alpha7 nicotinic acetylcholine receptors in mice. Psychopharmacology (Berl), 225(3):543-551.
| Cas No. | 357-70-0 | SDF | |
| 别名 | 加兰他敏; Galantamine | ||
| 化学名 | (4aS,6R,8aS)-3-methoxy-11-methyl-5,6,9,10,11,12-hexahydro-4aH-benzo[2,3]benzofuro[4,3-cd]azepin-6-ol | ||
| Canonical SMILES | [H][C@@]([C@@]1(C([H])=C2[H])C3=C(C([H])=C4[H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])(C([H])([H])[C@@]2([H])O[H])OC3=C4OC([H])([H])[H] | ||
| 分子式 | C17H21NO3 | 分子量 | 287.35 |
| 溶解度 | ≥ 14.4 mg/mL in DMSO, ≥ 45 mg/mL in EtOH with gentle warming, ≥ 14.43 mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
| 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 | 3.4801 mL | 17.4004 mL | 34.8008 mL |
| 5 mM | 0.696 mL | 3.4801 mL | 6.9602 mL |
| 10 mM | 0.348 mL | 1.74 mL | 3.4801 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。