Mianserin hydrochloride

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Chemical Structure| 21535-47-7 同义名 : 米安舍林盐酸盐 ;Org GB 94;Mianserin HCl
CAS号 : 21535-47-7
货号 : A128330
分子式 : C18H21ClN2
纯度 : 99+%
分子量 : 300.826
MDL号 : MFCD00055072
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
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

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].
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 <<
实验方案
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
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