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Atomoxetine HCI/盐酸托莫西汀 {[allProObj[0].p_purity_real_show]}

货号:A258704 同义名: Tomoxetine hydrochloride; (R)-Tomoxetine hydrochloride

Atomoxetine HCI是一种选择性的非兴奋性去甲肾上腺素再摄取抑制剂,具有认知增强作用,Ki 值分别为去甲肾上腺素 5 nM、5-羟色胺 77 nM、多巴胺 1451 nM。

Atomoxetine HCI/盐酸托莫西汀 化学结构 CAS号:82248-59-7
Atomoxetine HCI/盐酸托莫西汀 化学结构
CAS号:82248-59-7
Atomoxetine HCI/盐酸托莫西汀 3D分子结构
CAS号:82248-59-7
Atomoxetine HCI/盐酸托莫西汀 化学结构 CAS号:82248-59-7
Atomoxetine HCI/盐酸托莫西汀 3D分子结构 CAS号:82248-59-7
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Atomoxetine HCI/盐酸托莫西汀 纯度/质量文件 产品仅供科研

货号:A258704 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline HCl 98%
Cisatracurium besylate 96%
Yohimbine HCI 99+%
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Labetalol HCl 98+%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

99%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Carvedilol 99%
Doxazosin mesylate 99%
Tolazoline HCl 98%
Esmolol HCl 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

99%
Zenidolol HCl ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

98%
Acebutolol HCl 97+%
Carteolol HCl 98+%
Betaxolol 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

97%
Bisoprolol 97%
Sotalol HCl 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

99%
Metoprolol 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Atomoxetine HCI/盐酸托莫西汀 生物活性

靶点
  • 5-HT

    5-HT, Ki:77 nM

描述 Atomoxetine hydrochloride is a norepinephrine transporter (NET) inhibitor and also acts as an N-methyl-D-aspartate receptor (NMDAR) antagonist. In vivo, atomoxetine (3 mg/kg, intraperitoneal injection) seems to decrease glutamatergic transmission in a brain region-specific manner[3]. ICV (intracerebroventricularly) administration of atomoxetine at 200 – 250 nmol significantly reduced S-IRA (seizure-induced respiratory arrest) evoked by acoustic stimulation in DBA/1 mice. Peripheral atomoxetine administration at a dosage that reduces S-IRA (15 mg/kg, IP) slightly increased basal ventilation and the ventilatory response to 7% CO2[4].

Atomoxetine HCI/盐酸托莫西汀 细胞实验

Cell Line
Concentration Treated Time Description References
83NS cells 20 μM ATX reduced the expression of Notch2 and Hey1 and inhibited sphere-forming ability. Cell Commun Signal. 2024 Nov 5;22(1):532
U87R cells 20 μM 48 h ATX inhibited the proliferation of U87R cells and reduced the expression of EMT and stemness-related markers. Cell Commun Signal. 2024 Nov 5;22(1):532
U373R cells 20 μM 48 h ATX inhibited the proliferation of U373R cells and reduced the expression of EMT and stemness-related markers. Cell Commun Signal. 2024 Nov 5;22(1):532
Rat cortical neurons 0.75-50 μM 20 seconds To evaluate the antagonistic effect of atomoxetine on NMDA receptors, results showed that atomoxetine blocked NMDA-induced membrane currents in a non-competitive manner with an IC50 of 3.47 μM Br J Pharmacol. 2010 May;160(2):283-91
Xenopus oocytes expressing GIRK2 channels 12.4±1.5 μM (EC50) To investigate the inhibitory effects of atomoxetine on GIRK2 channels, results showed that atomoxetine reversibly reduced GIRK currents in a concentration-dependent manner. Neuropsychopharmacology. 2010 Jun;35(7):1560-9
Xenopus oocytes expressing GIRK1/GIRK4 channels 6.5±0.4 μM (EC50) To investigate the inhibitory effects of atomoxetine on GIRK1/GIRK4 channels, results showed that atomoxetine reversibly reduced GIRK currents in a concentration-dependent manner. Neuropsychopharmacology. 2010 Jun;35(7):1560-9
Xenopus oocytes expressing GIRK1/GIRK2 channels 10.9±1.3 μM (EC50) To investigate the inhibitory effects of atomoxetine on GIRK1/GIRK2 channels, results showed that atomoxetine reversibly reduced GIRK currents in a concentration-dependent manner. Neuropsychopharmacology. 2010 Jun;35(7):1560-9

Atomoxetine HCI/盐酸托莫西汀 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Dopamine transporter knockout (DAT-KO) rats Intraperitoneal injection 3 mg/kg Single dose, 30 minutes before testing To evaluate the effect of atomoxetine on the behavior and brain activity of DAT-KO rats. Results showed that atomoxetine significantly improved PPI and decreased repetitive behaviors in DAT-KO rats but did not affect hyperactivity or the number of errors. Additionally, ATX led to significant changes in power spectra and coherence of DAT-KO and wild type rats. Biomolecules. 2022 Oct 14;12(10):1484
Sprague Dawley rats Adolescent rat model Intraperitoneal injection 3 mg/kg Once daily for 21 days To assess the long-term effects of Atomoxetine on the transcriptional and translational processes of NET and NMDAR subunits. Results showed that Atomoxetine significantly reduced NET levels in the hippocampus and decreased protein levels of NMDAR subunit 2B in both the striatum and hippocampus. Drug Des Devel Ther. 2013 Dec 4;7:1433-46
BALB/c nude mice Subcutaneous xenograft model Intraperitoneal injection 20 mg/kg Once daily for 5 days ATX suppressed tumor growth in radioresistant GBM cells and reduced the expression of Notch2 and Hey1. Cell Commun Signal. 2024 Nov 5;22(1):532
Rats and rhesus monkeys 5-choice serial reaction time task (5C-SRTT) and eight-arm radial arm maze (RAM) task Intraperitoneal (rats), Intramuscular (monkeys) 0.3-3.0 mg/kg (rats), 0.03-1.0 mg/kg (monkeys) Single administration Atomoxetine improved attention and inhibitory response control in adult rats and spatial reference memory in adult rats. In aged monkeys, atomoxetine improved distractibility in a working/short-term memory task. Neuropharmacology. 2019 Sep 1;155:65-75
Long-Evans rats Adolescent rat attentional set-shifting task model Intraperitoneal injection 0.0, 0.1, 0.9 mg/kg/ml Administered 30 minutes before each test, lasting for 3 days To evaluate the effect of Atomoxetine on executive function in adolescent rats, particularly attentional set-shifting ability. The lowest dose (0.1 mg/kg/ml) significantly improved attentional set-shifting but had no effect on reversal learning. Dev Cogn Neurosci. 2011 Oct;1(4):552-9
C57BL/6 mice Nicotine withdrawal model Intraperitoneal injection 0.2 or 2.0 mg/kg Single administration, 20 min before training and testing Atomoxetine dose-dependently reversed the nicotine withdrawal-associated deficit in contextual fear conditioning, suggesting that nicotine withdrawal may be associated with changes in noradrenergic function, acetycholinergic function, and/or with changes in cell signaling cascades that are activated by both nicotine and norepinephrine. Neuropsychopharmacology. 2007 Sep;32(9):2011-9

Atomoxetine HCI/盐酸托莫西汀 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00191880 Attention Deficit Hyperactivit... 展开 >>y Disorder 收起 << Phase 3 Completed - Canada ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Calgary, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Edmonton, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician London, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Montreal, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Saskatoon, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Scarborough, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician St. Johns, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Toronto, Canada 收起 <<
NCT00286949 Parkinson's Disease Not Applicable Completed - United States, Maryland ... 展开 >> Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 收起 <<
NCT00286949 - Completed - -

Atomoxetine HCI/盐酸托莫西汀 参考文献

[1]Bymaster FP, Katner JS, 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 Nov;27(5):699-711.

[2]Zerbe RL, Rowe H, et al. Clinical pharmacology of tomoxetine, a potential antidepressant. J Pharmacol Exp Ther. 1985 Jan;232(1):139-43.

[3]Udvardi PT, Föhr KJ, Henes C, Liebau S, Dreyhaupt J, Boeckers TM, Ludolph AG. Atomoxetine affects transcription/translation of the NMDA receptor and the norepinephrine transporter in the rat brain--an in vivo study. Drug Des Devel Ther. 2013 Dec 4;7:1433-46.

[4]Zhao H, Cotten JF, Long X, Feng HJ. The effect of atomoxetine, a selective norepinephrine reuptake inhibitor, on respiratory arrest and cardiorespiratory function in the DBA/1 mouse model of SUDEP. Epilepsy Res. 2017 Nov;137:139-144.

Atomoxetine HCI/盐酸托莫西汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.13mL

3.43mL

1.71mL

34.27mL

6.85mL

3.43mL

Atomoxetine HCI/盐酸托莫西汀 技术信息

CAS号82248-59-7
分子式C17H22ClNO
分子量 291.82
SMILES Code CC1=CC=CC=C1O[C@@H](C2=CC=CC=C2)CCNC.[H]Cl
MDL No. MFCD06410992
别名 Tomoxetine hydrochloride; (R)-Tomoxetine hydrochloride; Atomoxetine (hydrochloride); LY 139603 HCl; Atomoxetine HCl; LY 139603
运输蓝冰
InChI Key LUCXVPAZUDVVBT-UNTBIKODSA-N
Pubchem ID 54840
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 105 mg/mL(359.82 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(171.34 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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