货号:A128330 同义名: 米安舍林盐酸盐 / Org GB 94;Mianserin HCl
Mianserin HCl is inverse agonist of H1 receptor and can be act as a psychoactive agent of the tetracyclic antidepressant.
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产品名称 | H1 receptor ↓ ↑ | H2 receptor ↓ ↑ | H3 receptor ↓ ↑ | H4 receptor ↓ ↑ | Histamine receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Hydroxyzine 2HCl | 99+% | ||||||||||||||||||
Cyclizine | ✔ | 97% | |||||||||||||||||
Loratadine |
+
B(0)AT2, IC50: 4 μM |
98% | |||||||||||||||||
Desloratadine |
++
Histamine H1 receptor, IC50: 51 nM |
98% | |||||||||||||||||
Doxylamine succinate | ✔ | 99% | |||||||||||||||||
Ebastine | ✔ | 98% | |||||||||||||||||
Tripelennamine HCl |
+
H1 receptor, IC50: 30 μM |
98% | |||||||||||||||||
Meclizine dihydrochloride | ✔ | 98% | |||||||||||||||||
Chlorpheniramine maleate |
+++
Histamine H1 receptor, IC50: 12 nM |
99% | |||||||||||||||||
Diphenhydramine HCl | ✔ | 99% | |||||||||||||||||
Alcaftadine |
++++
H1 receptor, pKi: 8.5 |
++
H2 receptor, pKi: 7.2 |
99%+ | ||||||||||||||||
Fexofenadine HCl |
++
Histamine H1 receptor, IC50: 246 nM |
99%+ | |||||||||||||||||
Bilastine |
+++
H1 receptor, Ki: 44.15 nM |
98% | |||||||||||||||||
Pemirolast potassium | ✔ | 98% | |||||||||||||||||
Bepotastine besilate |
+
Histamine H1 receptor, pIC50: 5.7 |
98% | |||||||||||||||||
Mizolastine |
+++
Histamine H1 receptor, IC50: 47 nM |
98% | |||||||||||||||||
Brompheniramine maleate | ✔ | 98% | |||||||||||||||||
Carbinoxamine maleate salt | ✔ | 99+% | |||||||||||||||||
Clemastine fumarate |
++++
Histamine H1 receptor, IC50: 3 nM |
98% | |||||||||||||||||
Ketotifen fumarate salt | ✔ | 95% | |||||||||||||||||
Rupatadine Fumarate |
++
Histamine H1 receptor, Ki: 102 nM |
PAFR | 98% | ||||||||||||||||
Famotidine | ✔ | 97% | |||||||||||||||||
Roxatidine Acetate HCl |
+
Histamine H2 receptor, IC50: 3.2 μM |
98% | |||||||||||||||||
Lafutidine | ✔ | 99% | |||||||||||||||||
Cimetidine | ✔ | 98% | |||||||||||||||||
Nizatidine |
++++
Histamine H2 receptor, IC50: 0.9 nM |
AChE | 98% | ||||||||||||||||
Ranitidine | ✔ | 99% | |||||||||||||||||
Betahistine |
+
Histamine H3 receptor, IC50: 1.9 μM |
98% | |||||||||||||||||
Ciproxifan maleate |
+++
Histamine H3 receptor, IC50: 9.2 nM |
99%+ | |||||||||||||||||
S 38093 |
++
human H3 receptor, Ki: 1.2 μM rat H3 receptor, Ki: 1.44 μM |
98% | |||||||||||||||||
JNJ-7777120 |
++++
Histamine H4 receptor, Ki: 4.5 nM |
98% | |||||||||||||||||
Azelastine HCl | ✔ | 98% | |||||||||||||||||
Epinastine HCl | ✔ | 98% | |||||||||||||||||
Levodropropizine | ✔ | 97% | |||||||||||||||||
Cyproheptadine hydrochloride | ✔ | 98% | |||||||||||||||||
Hesperetin | ✔ | 97% | |||||||||||||||||
Olopatadine HCl | ✔ | 98% | |||||||||||||||||
Mianserin hydrochloride | ✔ | 99+% | |||||||||||||||||
Buclizine 2HCl | ✔ | 97% | |||||||||||||||||
Latrepirdine 2HCl | ✔ | GluR | 98% | ||||||||||||||||
Cetirizine 2HCl | ✔ | 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 |
|
描述 | Mianserin Hydrochloride is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression. Mianserin (2 mg/kg s.c.) causes a modest increase of DOPAC (Dihydroxyphenylacetic acid) levels up to about 30% above base-line, which is statistically significant when compared to saline. Mianserin increases extracellular norepinephnne, but a comparison with desipramine and idazoxan showed that both NE reuptake inhibition and alpha-2 autoreceptor blockade contributed to the mianserin-induced increase in extracellular norepinephnne[3]. Mianserin (1, 5 and 10 mg/kg, SC) dose-dependently increases up to about 6 times extracellular dopamine in the medial prefrontal cortex of the rat. Mianserin also dose-dependently increases extracellular noradrenaline in the prefrontal cortex. Mianserin also dose-dependently increased extracellular noradrenaline in the prefrontal cortex[4]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00926835 | Major Depressive Disorder | Phase 4 | Terminated(due to patient recr... 展开 >>uitment difficulties) 收起 << | - | Korea, Republic of ... 展开 >> Clinical research center for depression Seoul, Korea, Republic of, 150713 收起 << |
NCT02336750 | Breast Cancer | Phase 3 | Recruiting | December 2019 | China ... 展开 >> Fudan University Cancer Hospital Recruiting Shanghai, China, 200032 Contact: Xichun Hu, MD,PhD 64175590 ext 5006 huxicun@gmail.com Contact: Jun Cao, MD 64175590 ext 5009 caojun1115lemon@163.com 收起 << |
NCT01764867 | Major Depressive Disorder | Phase 4 | Unknown | December 2014 | China ... 展开 >> Shanghai Mental Health Center Recruiting Shanghai, China, 200030 Contact: Zhiguo Wu, M.D. 862134289888 ext 3528 wu_zhiguo@yahoo.com.cn Principal Investigator: Yiru Fang, Ph.D., M.D. 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.32mL 0.66mL 0.33mL |
16.62mL 3.32mL 1.66mL |
33.24mL 6.65mL 3.32mL |
CAS号 | 21535-47-7 |
分子式 | C18H21ClN2 |
分子量 | 300.826 |
别名 | 米安舍林盐酸盐 ;Org GB 94;Mianserin HCl |
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,2-8°C |
溶解度 |
DMSO: 50 mg/mL(166.21 mM),配合低频超声助溶,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: 25 mg/mL(83.1 mM),配合低频超声,并水浴加热至45℃助溶 |
动物实验配方 |
PO 0.5% CMC-Na 15 mg/mL suspension |