| Description | Atomoxetine (HSDB 7352) is a selective norepinephrine inhibitor that may cause an increase in blood pressure by increasing norepinephrine concentrations in peripheral sympathetic neurons .Atomoxetine is a highly selective antagonist of presynaptic norepinephrine transporters with little or no affinity for other norepinephrine receptors or other neurotransmitter transporters or receptors, but has little or no affinity for 5- hydroxytryptamine transporter. Atomoxetine selectively inhibits reuptake of norepinephrine and can be used to treat adolescents with ADHD and chronic tics. |
| In vitro | Atomoxetine (Tomoxetine)在tsA201细胞中对人心脏钠通道(hNav1.5)表现出状态和剂量依赖性的作用，作用浓度范围为1到100 µM，暴露时间为0.5到20秒。[2] |
| In vivo | 将Atomoxetine (Tomoxetine)以0.3-3 mg/kg（i.p.）剂量给予雄性Sprague-Dawley大鼠，持续0-4小时，可以导致额外细胞去甲肾上腺素和多巴胺水平增加三倍，同时在前额叶皮层观察到Fos表达增加。[1] 此外，Atomoxetine (Tomoxetine)以0.1-5 mg/kg（i.p.和p.o.）剂量在14天内给予自发性高血压大鼠，显示出改善大鼠ADHD相关行为的潜力。[3] |
| Target activity | Dopamine:1451 nM, 5-HT:77 nM, Norepinephrine:5 nM |
| Synonyms | Tomoxetine, HSDB7352, HSDB-7352, HSDB 7352 |
| molecular weight | 255.35 |
| Molecular formula | C17H21NO |
| CAS | 83015-26-3 |
| Storage | store at low temperature|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: Soluble |
| References | 1. Turner M, et al. Effects of atomoxetine on locomotor activity and impulsivity in the spontaneously hypertensive rat. Behav Brain Res. 2013;243:28-37. 2. Föhr KJ, et al. Block of Voltage-Gated Sodium Channels by Atomoxetine in a State- and Use-dependent Manner. Front Pharmacol. 2021;12:622489. 3. Bymaster FP, 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. Neuropsychopharmacology. 2002;27(5):699-711. 4. Mosholder AD, et al. Incidence of Heart Failure and Cardiomyopathy Following Initiation of Medications for Attention-Deficit/Hyperactivity Disorder: A Descriptive Study. J Clin Psychopharmacol. 2018;38(5):505-508. 5. Cortese S, et al. Comparative efficacy and tolerability of medications for attention-deficit hyperactivity disorder in children, adolescents, and adults: a systematic review and network meta-analysis. Lancet Psychiatry. 2018;5(9):727-738. 6. Froehlich T, et al. Using ADHD Medications to Treat Coexisting ADHD and Reading Disorders: A Systematic Review. Clin Pharmacol Ther. 2018;104(4):619-637. 7. van den Brink RL, et al. Amplification and Suppression of Distinct Brain-wide Activity Patterns by Catecholamines. Journal of Neuroscience. 2018;38(34): 7476-7491. |