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Maprotiline hydrochloride

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Chemical Structure| 10347-81-6 同义名 : 马替普林盐酸盐 ;Maprotiline (hydrochloride) (CRM);Maprotiline HCl;Ba 34276
CAS号 : 10347-81-6
货号 : A457280
分子式 : C20H24ClN
纯度 : 98%
分子量 : 313.864
MDL号 : MFCD00079464
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 <<
实验方案
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
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.