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盐酸马普替林 /Maprotiline hydrochloride {[allProObj[0].p_purity_real_show]}

货号:A457280 同义名: 马替普林盐酸盐 / Maprotiline (hydrochloride) (CRM);Maprotiline HCl

Maprotiline HCl is a bridged-ring tetracyclic antidepressant with adrenergic activity and sedative properties, exerting its effect by blocking the re-uptake of norepinephrine, thereby increasing the synaptic concentration of norepinephrine in the central nervous system and subsequently prolonging the action of norepinephrine on central receptors.

Maprotiline hydrochloride 化学结构 CAS号:10347-81-6
Maprotiline hydrochloride 化学结构
CAS号:10347-81-6
Maprotiline hydrochloride 3D分子结构
CAS号:10347-81-6
Maprotiline hydrochloride 化学结构 CAS号:10347-81-6
Maprotiline hydrochloride 3D分子结构 CAS号:10347-81-6
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Maprotiline hydrochloride 纯度/质量文件 产品仅供科研

货号:A457280 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 hydrochloride 98%
Cisatracurium besylate 98%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-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%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

97%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Doxazosin mesylate 98%
Tolazoline HCl 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

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。

Maprotiline hydrochloride 生物活性

靶点
  • Adrenergic Receptor

描述 Maprotiline (Hydrochloride), selective NA reuptake inhibitor, a tetracyclic antidepressant with sedative properties, exhibits strong inhibitory effects on norepinephrine uptake across nerve cell membranes but interferes relatively little with serotoninergic mechanisms[3]. Maprotiline bounds to the full-length recombinant sGC (Soluble guanylate cyclase) with a high affinity (KD = 0.307 μM). Moreover, in a monocrotaline rat model of PAH (Pulmonary arterial hypertension), maprotiline (ip, 10 mg/kg once daily) reduced pulmonary hypertension, inhibited the development of right ventricular hypertrophy and pathological changes of the pulmonary vascular remodeling[4].

Maprotiline hydrochloride 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
NCT02873234 - Recruiting May 2020 China, Beijing ... 展开 >> The Third Affiliated Hospital of Beijing University of Chinese Medicine Recruiting Beijing, Beijing, China, 100029 Contact: Wenjun Sun, MD, PHD    +86 18910259376    doctorsunwenjun@126.com 收起 <<
NCT02374567 Dementia Depr... 展开 >>ession Schizophrenia Psychosomatic Disorders Anxiety Disorders 收起 << Phase 3 Terminated - Germany ... 展开 >> Bezirkskrankenhaus Augsburg Augsburg, Germany Krankenhaus Hedwigshöhe Berlin, Germany Hannover Medical School Hannover, Germany, 30625 Asklepios Fachklinikum Lübben Lübben, Germany Asklepios Fachklinikum Teupitz Teupitz, Germany 收起 <<
NCT00704860 Major Depression Phase 4 Completed - Canada, Ontario ... 展开 >> University of Ottawa Institute of Mental Health Research Ottawa, Ontario, Canada, K1Z 7K4 收起 <<

Maprotiline hydrochloride 参考文献

[1]Ferrer-Villada T, Navarro-Polanco RA, et al. Inhibition of cardiac HERG potassium channels by antidepressant maprotiline. Eur J Pharmacol. 2006 Feb 15;531(1-3):1-8.

[2]Arenas MC, Vinader-Caerols C, et al. Are the effects of the antidepressants amitriptyline, maprotiline, and fluoxetine on inhibitory avoidance state-dependent? Behav Brain Res. 2006 Jan 6;166(1):150-8.

[3]Wells BG, Gelenberg AJ. Chemistry, pharmacology, pharmacokinetics, adverse effects, and efficacy of the antidepressant maprotiline hydrochloride. Pharmacotherapy. 1981 Sep-Oct;1(2):121-39.

[4]Tong Y, Jiao Q, Liu Y, Lv J, Wang R, Zhu L. Maprotiline Prevents Monocrotaline-Induced Pulmonary Arterial Hypertension in Rats. Front Pharmacol. 2018 Sep 21;9:1032.

Maprotiline hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.93mL

3.19mL

1.59mL

31.86mL

6.37mL

3.19mL

Maprotiline hydrochloride 技术信息

CAS号10347-81-6
分子式C20H24ClN
分子量 313.864
别名 马替普林盐酸盐 ;Maprotiline (hydrochloride) (CRM);Maprotiline HCl;Ba 34276
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 85 mg/mL(270.82 mM),配合低频超声,并水浴加热至45℃助溶,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: 2 mg/mL(6.37 mM),配合低频超声助溶

动物实验配方
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