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盐酸米安色林 /Mianserin hydrochloride {[allProObj[0].p_purity_real_show]}

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.

Mianserin hydrochloride 化学结构 CAS号:21535-47-7
Mianserin hydrochloride 化学结构
CAS号:21535-47-7
Mianserin hydrochloride 3D分子结构
CAS号:21535-47-7
Mianserin hydrochloride 化学结构 CAS号:21535-47-7
Mianserin hydrochloride 3D分子结构 CAS号:21535-47-7
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Mianserin hydrochloride 纯度/质量文件 产品仅供科研

货号:A128330 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 98%
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。

Mianserin hydrochloride 生物活性

靶点
  • Histamine receptor

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].

Mianserin 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
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 <<

Mianserin hydrochloride 参考文献

[1]Olianas MC, Dedoni S, et al. The atypical antidepressant mianserin exhibits agonist activity at κ-opioid receptors. Br J Pharmacol. 2012 Nov;167(6):1329-41.

[2]de Boer TH, Nefkens F, et al. Differences in modulation of noradrenergic and serotonergic transmission by the alpha-2 adrenoceptor antagonists, mirtazapine, mianserin and idazoxan. J Pharmacol Exp Ther. 1996 May;277(2):852-60.

[3]de Boer TH, Nefkens F, van Helvoirt A, van Delft AM. Differences in modulation of noradrenergic and serotonergic transmission by the alpha-2 adrenoceptor antagonists, mirtazapine, mianserin and idazoxan. J Pharmacol Exp Ther. 1996 May;277(2):852-60

[4]Tanda G, Bassareo V, Di Chiara G. Mianserin markedly and selectively increases extracellular dopamine in the prefrontal cortex as compared to the nucleus accumbens of the rat. Psychopharmacology (Berl). 1996 Jan;123(2):127-30

[5]Rocha B, Rigo M, Di Scala G, Sandner G, Hoyer D. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31

Mianserin hydrochloride 实验方案

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

Mianserin hydrochloride 技术信息

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

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