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.
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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。 |
靶点 |
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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]. |
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 << |
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 |
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 |