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 organic compound classified as a selective norepinephrine reuptake inhibitor (NRI). Distinguished by its unique chemical structure and high solubility in water, Atomoxetine Hydrochloride is widely utilized in biochemical and pharmacological research. Its mechanism of action centers on selectively inhibiting the presynaptic norepinephrine transporter, thereby increasing extracellular levels of norepinephrine in the central nervous system. This property makes it a valuable tool for exploring monoaminergic pathways and neurotransmitter regulation. Atomoxetine Hydrochloride's stability and compatibility with various assay systems further enhance its utility in experimental protocols that require precise modulation of noradrenergic signaling.
Neurotransmitter Transporter Studies: Atomoxetine Hydrochloride is extensively employed in laboratory investigations aimed at elucidating the function and regulation of norepinephrine transporters. By selectively blocking these transporters, researchers can assess the dynamics of norepinephrine uptake and release in neuronal cell models. This facilitates a deeper understanding of synaptic transmission, transporter kinetics, and the interplay between different monoamine systems. Its application in transporter binding assays and uptake inhibition studies provides critical reference data for the development of new pharmacological agents targeting neurotransmitter reuptake mechanisms.
Behavioral Neuroscience Research: In preclinical behavioral models, Atomoxetine or its hydrochloride salt is used to modulate noradrenergic tone and study its effects on cognitive processes such as attention, impulsivity, and executive function. Researchers utilize it to induce or ameliorate specific behavioral phenotypes in animal models, allowing for the dissection of the neurochemical substrates underlying complex behaviors. Its selective action enables the isolation of norepinephrine's contribution to behavioral outcomes, which is particularly valuable in comparative studies involving other neurotransmitter systems.
Drug-Drug Interaction Analysis: Atomoxetine Hydrochloride serves as a reference compound in drug-drug interaction studies, particularly those focusing on cytochrome P450-mediated metabolism. By examining its metabolic profile in the presence of other compounds, researchers can identify potential interactions and elucidate the role of specific CYP isoforms in its biotransformation. This information is crucial for predicting metabolic liabilities and optimizing the design of novel therapeutic agents with favorable pharmacokinetic properties.
Pharmacokinetic and Bioavailability Studies: The compound is frequently used in in vitro and in vivo models to investigate absorption, distribution, metabolism, and excretion (ADME) characteristics. Atomoxetine Hydrochloride's well-characterized metabolic pathways provide a framework for evaluating the impact of genetic or environmental factors on drug disposition. Studies utilizing this molecule contribute to a broader understanding of the determinants of oral bioavailability and systemic exposure, which inform rational drug design and dosing strategies for related compounds.
Neuropharmacological Mechanism Elucidation: Researchers leverage Atomoxetine Hydrochloride to probe the downstream effects of enhanced norepinephrine signaling on neuronal plasticity, synaptic connectivity, and intracellular signaling cascades. By modulating noradrenergic activity, it is possible to dissect the contributions of this neurotransmitter to neuroadaptive processes and neurodevelopmental trajectories. Such studies are instrumental in mapping the cellular and molecular mechanisms that underlie neuropsychiatric and neurodevelopmental conditions, providing foundational insights for future research endeavors. Atomoxetine Hydrochloride's versatility and specificity make it an indispensable reagent in the toolkit of neuroscientists and pharmacologists seeking to unravel the complexities of noradrenergic function and its broader implications in brain physiology.
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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