Atomoxetine HCl
(Synonyms: 盐酸托莫西汀; Tomoxetine hydrochloride; (R)-Tomoxetine hydrochloride; LY 139603) 目录号 : GC10274
Atomoxetine HCl是一种强效、选择性的去甲肾上腺素摄取抑制剂，对去甲肾上腺素、血清素（5-HT）和多巴胺（DA）的Ki值分别为5、77和1451nM。
Cas No.:82248-59-7
Sample solution is provided at 25 µL, 10mM.
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Atomoxetine HCl is a potent and selective norepinephrine uptake inhibitor, with Ki values of 5, 77, and 1451nM for norepinephrine, serotonin (5-HT) and dopamine (DA) [1]. Atomoxetine HCl inhibits cloned human Ether-à-Go-Go-Related Gene (hERG) channels, with an IC50 value of 6.3µM[2]. Atomoxetine HCl can regulate the gene expression of neurotransmitter receptors and synaptic signaling molecules in fruit flies, and increase the locomotor activity of wild-type fruit flies[3]. Atomoxetine HCl has been widely used in animal models of Attention-Deficit/Hyperactivity Disorder (ADHD) to improve hyperactivity symptoms[4].
In vitro, Atomoxetine HCl treatment (50μM) for 7 days induced cell death in human neuron-like cells, resulting in a significant increase in mitochondrial ROS production[5]. Treatment with 50ng/ml Atomoxetine HCl for 24 hours significantly reduced the expression level of 8-hydroxyguanine glycosylase 1 (hOGG1) in U-937 cells[6]. In differentiated human SH-SY5Y neuroblastoma cells treated with 50μM Atomoxetine HCl for 7 days, the expressions of SDHA and COX-I were significantly downregulated, and mitochondrial fusion and mitochondrial division were disrupted[7].
In vivo, Atomoxetine HCl treatment for 10 days at a dose of 3mg/kg/day by intraperitoneal, intraperitoneal improved the spatial reference memory of adult rats, and enhanced the attention and inhibitory response control ability of adult rats[8]. Continuous intraperitoneal injection of Atomoxetine HCl (30mg/kg) once daily for 3 consecutive days can prevent ischemic neuronal death in the hippocampus of gerbils and significantly reduce the activation of glial cells caused by ischemia[9].
References:
[1] Bymaster F P, Katner J S, Nelson D L, et al. Atomoxetine increases extracellular levels of norepinephrine and dopamine in prefrontal cortex of rat: a potential mechanism for efficacy in attention deficit/hyperactivity disorder[J]. Neuropsychopharmacology, 2002, 27(5): 699-711.
[2] Scherer D, Hassel D, Bloehs R, et al. Selective noradrenaline reuptake inhibitor atomoxetine directly blocks hERG currents[J]. British journal of pharmacology, 2009, 156(2): 226-236.
[3] Qu S, Zhou X, Wang Z, et al. The effects of methylphenidate and atomoxetine on Drosophila brain at single-cell resolution and potential drug repurposing for ADHD treatment[J]. Molecular Psychiatry, 2024, 29(1): 165-185.
[4] Moon S J, Kim C J, Lee Y J, et al. Effect of atomoxetine on hyperactivity in an animal model of attention-deficit/hyperactivity disorder (ADHD)[J]. PLoS One, 2014, 9(10): e108918.
[5] Corona J C, Carreón-Trujillo S, González-Pérez R, et al. Atomoxetine produces oxidative stress and alters mitochondrial function in human neuron-like cells[J]. Scientific reports, 2019, 9(1): 13011.
[6] Schmidt A J, Clement H W, Gebhardt S, et al. Impact of psychostimulants and atomoxetine on the expression of 8-hydroxyguanine glycosylase 1 in human cells[J]. Journal of neural transmission, 2010, 117(6): 793-797.
[7] Carreón-Trujillo S, Vázquez-González D, Corona J C. Atomoxetine Decreases Mitochondrial Biogenesis, Fission and Fusion In Human Neuron-like Cells But Does Not Alter Antioxidant Defences[J]. Cell Biochemistry and Biophysics, 2023, 81(1): 105-115.
[8] Callahan P M, Plagenhoef M R, Blake D T, et al. Atomoxetine improves memory and other components of executive function in young-adult rats and aged rhesus monkeys[J]. Neuropharmacology, 2019, 155: 65-75.
[9] Park J H, Shin B N, Chen B H, et al. Neuroprotection and reduced gliosis by atomoxetine pretreatment in a gerbil model of transient cerebral ischemia[J]. Journal of the neurological sciences, 2015, 359(1-2): 373-380.
Atomoxetine HCl是一种强效、选择性的去甲肾上腺素摄取抑制剂，对去甲肾上腺素、血清素（5-HT）和多巴胺（DA）的Ki值分别为5、77和1451nM[1]。Atomoxetine HCl能抑制克隆的人Ether-à-Go-Go相关基因（hERG）通道，IC50值为6.3µM[2]。Atomoxetine HCl可调节果蝇体内神经递质受体和突触信号分子的基因表达，并增加野生型果蝇的运动活性[3]。Atomoxetine HCl已被广泛用于注意力缺陷/多动障碍（ADHD）的动物模型，以改善多动症状[4]。
在体外，使用50µM的Atomoxetine HCl处理7天，可诱导人神经元样细胞死亡，导致线粒体ROS生成显著增加[5]。使用50ng/ml的Atomoxetine HCl处理24小时，显著降低了U-937细胞中8-羟基鸟嘌呤糖苷酶1（hOGG1）的表达水平[6]。在使用50µM的Atomoxetine HCl处理7天的分化人SH-SY5Y神经母细胞瘤细胞中，SDHA和COX-I的表达显著下调，线粒体融合与分裂过程被破坏[7]。
在体内，每日腹腔注射3mg/kg剂量的Atomoxetine HCl，持续10天，改善了成年大鼠的空间参考记忆，并增强了注意力和抑制反应控制能力[8]。连续3天每日腹腔注射Atomoxetine HCl（30mg/kg），可预防沙土鼠海马中的缺血性神经元死亡，并显著减轻由缺血引起的胶质细胞活化[9]。
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells |
Preparation Method | SH-SY5Y cells were cultured in DMEM/F12 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) and streptomycin(100µg/ml)/penicillin/(100U/ml) at 37°C in a humidified environment with 5% CO2. The cells were placed in a medium containing 2% FBS and treated with 10µM retinoic acid (RA), with the medium being replaced every 2 days. The untreated differentiated cells served as the control group. The differentiated cells were treated with 1, 5, 10, 20, and 50µM Atomoxetine HCl for 7 days. After Atomoxetine HCl treatment, the differentiated SH-SY5Y cells were collected and lysed with RIPA lysis buffer containing a mixture of protease and phosphatase inhibitors for immunoblot analysis. |
Reaction Conditions | 1, 5, 10, 20, and 50µM; 7 days |
Applications | Atomoxetine HCl treatment downregulated the mitochondrial fusion markers OPA1 and MFN2 as well as the fission markers DRP1 and Fis1 in the differentiated SH-SY5Y cells. |
| Animal experiment [2]: | |
Animal models | Male Mongolian gerbils |
Preparation Method | Male Mongolian gerbils (6 months old, weighing 75-80 grams) were raised under pathogen-free (SPF) conditions, with a temperature of 23℃, humidity of 60%, a light/dark cycle of 12 hours/12 hours, and had free access to food and water. Group the gerbils as follows: 1) The sham operation group, which received sham surgery; 2) The ischemia-preconditioned normal saline group, which received normal saline before ischemia-reperfusion; 3) The 30mg/kg Atomoxetine HCl ischemia-preconditioned group, which was given 30mg/kg Atomoxetine HCl before ischemia-reperfusion. Atomoxetine HCl is dissolved in normal saline and is administered intraperitoneally once a day for 3 consecutive days before and after ischemia surgery: the last pre-treatment is performed 30 minutes before the surgery. After ischemia-reperfusion, the brain tissue is collected for analysis. |
Dosage form | 30mg/kg/day for 3 days; i.p. |
Applications | Atomoxetine HCl treatment prevented ischemic neuronal death in the hippocampus of gerbils and significantly reduced the activation of glial cells caused by ischemia. |
References: | |
| Cas No. | 82248-59-7 | SDF | |
| 别名 | 盐酸托莫西汀; Tomoxetine hydrochloride; (R)-Tomoxetine hydrochloride; LY 139603 | ||
| 化学名 | (3R)-N-methyl-3-(2-methylphenoxy)-3-phenylpropan-1-amine;hydrochloride | ||
| Canonical SMILES | CC1=CC=CC=C1OC(CCNC)C2=CC=CC=C2.Cl | ||
| 分子式 | C17H22ClNO | 分子量 | 291.82 |
| 溶解度 | ≥ 14.35mg/mL in DMSO | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4268 mL | 17.1338 mL | 34.2677 mL |
| 5 mM | 685.4 μL | 3.4268 mL | 6.8535 mL |
| 10 mM | 342.7 μL | 1.7134 mL | 3.4268 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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