Atomoxetine (brand name Strattera) is a norepinephrine reuptake inhibitor approved for the treatment of attention deficit hyperactivity disorder (ADHD).This compound is manufactured, marketed, and sold in the United States as the hydrochloride salt (atomoxetine HCl) under the brand name Strattera.
CAT No: 10-101-111
CAS No:82248-59-7
Synonyms/Alias:LY-135252; LY-139602; LY-139603; Tomoxetine Hydrochloride; (R)-(-)-N-Methyl-3-(o-tolyloxy)-3-phenylpropylamine · HCl; (R)-(-)-N-Methyl-γ-(2-methylphenoxy)-benzenepropanamine · HCl
Chemical Name:(3R)-N-methyl-3-(2-methylphenoxy)-3-phenylpropan-1-amine;hydrochloride
Atomoxetine Hydrochloride is a synthetic small molecule classified as a selective norepinephrine reuptake inhibitor (NRI). Structurally, it is a hydrochloride salt form of atomoxetine, which is characterized by its ability to modulate synaptic concentrations of norepinephrine in the central nervous system. Its mechanism of action and pharmacological profile have made it a valuable compound for neuroscience research, particularly in the study of monoaminergic signaling and neurobehavioral processes. The compound's specificity for norepinephrine transporters, combined with minimal affinity for other monoamine systems, has positioned it as a reference molecule in both academic and industrial research settings investigating attention, cognition, and neurotransmitter regulation.
Neurotransmitter Transporter Research: Atomoxetine Hydrochloride is extensively utilized in studies focused on the function and regulation of the norepinephrine transporter (NET). By selectively inhibiting NET, it allows researchers to dissect the role of norepinephrine reuptake in synaptic transmission, neuronal excitability, and network-level modulation. This property is instrumental for elucidating the molecular mechanisms underlying attention, arousal, and stress responses in both in vitro and in vivo models.
Behavioral Pharmacology: The compound serves as a powerful tool in behavioral neuroscience for investigating the impact of altered norepinephrine signaling on cognitive and behavioral outcomes. Experimental paradigms frequently employ it to probe the neurobiological substrates of attention, impulsivity, and executive function. Its use enables the assessment of how selective NET inhibition influences learning, memory processes, and behavioral phenotypes in animal models, supporting the development of new hypotheses regarding neuropsychiatric conditions.
Drug Metabolism and Pharmacokinetics: Atomoxetine Hydrochloride is widely applied in pharmacokinetic profiling and metabolic pathway elucidation. Studies involving this compound help characterize absorption, distribution, metabolism, and excretion (ADME) parameters, as well as the identification of active metabolites. This information is critical for understanding interindividual variability in drug response and for optimizing dosing strategies in preclinical models.
Receptor Binding and Selectivity Studies: The compound is frequently employed in receptor binding assays to validate its selectivity profile and to differentiate NET-mediated effects from those mediated by other monoamine transporters, such as the dopamine and serotonin transporters. Such studies provide clarity on the molecular interactions responsible for its pharmacological specificity, supporting the rational design of next-generation norepinephrine reuptake inhibitors and related neuroactive agents.
Neurochemical Assays: Atomoxetine Hydrochloride is used in a variety of neurochemical assays to quantify changes in extracellular norepinephrine levels and to monitor downstream signaling pathways. Techniques such as microdialysis, high-performance liquid chromatography (HPLC), and mass spectrometry leverage its selective action to map neurotransmitter dynamics in real time. These applications advance the understanding of noradrenergic system function and facilitate the identification of biomarkers relevant to neuropsychiatric research.
In the studies reported here, the ability of atomoxetine hydrochloride (Strattera) to inhibit or induce the metabolic capabilities of selected human isoforms of cytochrome P450 was evaluated. Initially, the potential of atomoxetine and its two metabolites, N-desmethylatomoxetine and 4-hydroxyatomoxetine, to inhibit the metabolism of probe substrates for CYP1A2, CYP2C9, CYP2D6, and CYP3A was evaluated in human hepatic microsomes. Although little inhibition of CYP1A2 and CYP2C9 activity was observed, inhibition was predicted for CYP3A (56% predicted inhibition) and CYP2D6 (60% predicted inhibition) at concentrations representative of high therapeutic doses of atomoxetine. The ability of atomoxetine to induce the catalytic activities of CYP1A2 and CYP3A in human hepatocytes was also evaluated; however, atomoxetine did not induce either isoenzyme. Based on the potential of interaction from the in vitro experiments, drug interaction studies in healthy subjects were conducted using probe substrates for CYP2D6 (desipramine) in CYP2D6 extensive metabolizer subjects and CYP3A (midazolam) in CYP2D6 poor metabolizer subjects. Single-dose pharmacokinetic parameters of desipramine (single dose of 50 mg) were not altered when coadministered with atomoxetine (40 or 60 mg b.i.d. for 13 days). Only modest changes (approximately 16%) were observed in the plasma pharmacokinetics of midazolam (single dose of 5 mg) when coadministered with atomoxetine (60 mg b.i.d. for 12 days). Although at high therapeutic doses of atomoxetine inhibition of CYP2D6 and CYP3A was predicted, definitive in vivo studies clearly indicate that atomoxetine administration with substrates of CYP2D6 and CYP3A does not result in clinically significant drug interactions.
Sauer J M, Long A J, Ring B, et al. Atomoxetine hydrochloride: clinical drug-drug interaction prediction and outcome[J]. Journal of Pharmacology and Experimental Therapeutics, 2004, 308(2): 410-418.
Attention-deficit/hyperactivity disorder (ADHD) occurs in approximately 3% to 10% of the pediatric population. Most of the drugs typically used to treat ADHD are stimulants, which, because of their addictive properties and potential for abuse, are controlled substances. Although these drugs are the mainstay of treatment for ADHD, nearly one third of patients may not respond to or be able to tolerate them. Atomoxetine hydrochloride, a nonstimulant approved by the US Food and Drug Administration for the treatment of ADHD, may provide an alternative to the use of stimulants.
Caballero J, Nahata M C. Atomoxetine hydrochloride for the treatment of attention-deficit/hyperactivity disorder[J]. Clinical therapeutics, 2003, 25(12): 3065-3083.
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