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米尔塔扎平 /Mirtazapine {[allProObj[0].p_purity_real_show]}

货号:A266101 同义名: 米氮平 / 6-Azamianserin;Org3770

Mirtazapine is a potent tetracyclic antidepressant.

Mirtazapine 化学结构 CAS号:85650-52-8
Mirtazapine 化学结构
CAS号:85650-52-8
Mirtazapine 3D分子结构
CAS号:85650-52-8
Mirtazapine 化学结构 CAS号:85650-52-8
Mirtazapine 3D分子结构 CAS号:85650-52-8
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Mirtazapine 纯度/质量文件 产品仅供科研

货号:A266101 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

98%
Venlafaxine 98%
Fluvoxamine maleate 99%
Iloperidone 98%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 98%
Fluoxetine HCl 99.5%
Paroxetine hydrochloride AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

99%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

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。

Mirtazapine 生物活性

靶点
  • 5-HT

描述 Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) that acts by antagonizing the adrenergic alpha2-autoreceptors and alpha2-heteroreceptors as well as by blocking 5-HT2 and 5-HT3 receptors. It enhances the release of norepinephrine and 5-HT1A-mediated serotonergic transmission. In vitro studies suggest that mirtazapine is unlikely to cause clinically significant drug-drug interactions. Dry mouth, sedation, and increases in appetite and body weight are the most common adverse effects. Mirtazapine also appears to be useful in patients suffering from depression comorbid with anxiety symptoms and sleep disturbance. It seems to be safe and effective during long-term use[3]. Mirtazapine seems to be safe in pregnancy, especially regarding incidence of congenital malformations[4]. A large-scale controlled evaluation is warranted to substantiate clinical utility of off-label use of mirtazapine (7.5 mg) for patients with AAA (antipsychotic-associated akathisia) [5]. Mirtazapine significantly improved both nausea and vomiting in gastroparetics after 2 and 4 weeks of treatment. Side effects led to treatment self-cessation in a fifth of patients[6].

Mirtazapine 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
NCT01216371 Renal Cell Carcinoma ... 展开 >> Pulmonary Metastases 收起 << Phase 2 Unknown October 2015 Germany ... 展开 >> Universitätsmedizin Charité Berlin Not yet recruiting Berlin, Germany, 10117 Contact: Steffen Weikert, Priv. Doz. Dr. med.    030/84 45-40 84       Principal Investigator: Steffen Weikert, Priv. Doz. Dr. med.          Sub-Investigator: Kempkensteffen Carsten, Dr. med.          Sub-Investigator: Jonas Busch, Dr. med.          Sub-Investigator: Jan Gregor, Dr. med.          Sub-Investigator: Jens Neudecker, Dr. med.          Sub-Investigator: Jens C. Rückert, Dr. med.          Sub-Investigator: Gertrud Feldmann          Franziskus Krankenhaus Not yet recruiting Berlin, Germany, 10787 Contact: Jörg Neymeyer, Dr. med.    030/26 38-38 01       Principal Investigator: Jörg Neymeyer, Dr. med.          Sub-Investigator: Thomas Wülfing, Dr. med.          Helios Klinikum Emil von Behring Not yet recruiting Berlin, Germany, 14165 Contact: Kollmeier Jens, Dr. med.    030/81 02-14 47       Sub-Investigator: Jens Kollmeier, Dr. med.          Sub-Investigator: Bettina Schlolaut, Dr. med.          university hospital of Düsseldorf Recruiting Düsseldorf, Germany, 40255 Contact: Peter Albers, Prof. Dr. med.    0211/811-81 10       Principal Investigator: Peter Albers, Prof. Dr. med.          Sub-Investigator: Jasper Decoene          Sub-Investigator: Zenginli Hakan          Sub-Investigator: Claus F. Eisenberger, Prof. Dr. med.          Sub-Investigator: Wolfram T. Knoefel, Prof. Dr. med.          Sub-Investigator: Almut Diem          university hospital of Essen Recruiting Essen, Germany, 45122 Contact: Herbert Rübben, Prof. Dr. med.    0201/723-32 10       Principal Investigator: Herbert Rübben, Prof. Dr. med.          Sub-Investigator: Marcus Schenk, Dr. med.          Sub-Investigator: Farnk vom Dorp, Dr. med.          Sub-Investigator: Min Ju, Dr. med.          Sub-Investigator: Stephan Tschirdewahn          Sub-Investigator: Michaela Löbert          Ruhrlandklinik Department of Thoracic Surgery Not yet recruiting Essen, Germany, 45239 Contact: Christiane Zimmermann    0201/433-43 24       Sub-Investigator: Georgios Stamatis, Prof. Dr. med.          Sub-Investigator: Stefan Welter, Dr. med.          Sub-Investigator: Silvia Fechner, Dipl. med.          university hospital of Freiburg Recruiting Freiburg, Germany, 79106 Contact: Ulrich Wetterauer, Prof. Dr. med.    0761/270-2891       Principal Investigator: Ulrich Wetterauer, Prof. Dr. med.          Sub-Investigator: Christian Leiber, Dr. med.          Sub-Investigator: Christian Stremmel, Prof. Dr. med.          Sub-Investigator: Jutta Günter, Dr. med.          university Hospital of Heidelberg Recruiting Heidelberg, Germany, 69119 Contact: Markus Hohenfellner, Prof. Dr. med.    06221/56-63 21       Principal Investigator: Markus Hohenfellner, Prof. Dr. med.          Sub-Investigator: Pahernick Sascha, Priv. Doz. Dr. med.          Sub-Investigator: Gencay Hatiboglu, Dr. med.          Sub-Investigator: Johannes Huber, Dr. Dr. med.          Sub-Investigator: Joachim Pfannschmidt, Priv. Doz. Dr. med.          Sub-Investigator: Hendrik Dienemann, Prof. Dr. med.          urological hospital of Maria Hilf Krankenhaus Krefeld Recruiting Krefeld, Germany, 47805 Contact: Susanne Krege, Priv. Doz. Dr. med.    02151/334-52 74       Principal Investigator: Susanne Krege, Priv. Doz. Dr. med.          Sub-Investigator: Florian Hartmann, Dr. med.          Hospital of Großhadern Not yet recruiting München, Germany, 81377 Contact: Michael Staehler, Dr. med.    089/70 95-0       Principal Investigator: Michael Staehler, Dr. med.          Sub-Investigator: Cordula Nordhaus, Dr. med.          Sub-Investigator: Philipp Nuhn, Dr. med.          Sub-Investigator: Hauke Winter, Priv. Doz. Dr. med.          Sub-Investigator: Rudolf Hatz, Prof. Dr. med.          Sub-Investigator: Sylvia Dondl          Dr.-Horst-Schmidt-Kliniken GmbH Recruiting Wiesbaden, Germany, 65199 Contact: Norbert Frickhofen, Prof. Dr. med.    0611/43-30 09       Principal Investigator: Norbert Frickhofen, Prof. Dr. med.          Sub-Investigator: Bernd Jung, Dr. med.          Sub-Investigator: Heinz G. Fuhr, Dr. med.          Sub-Investigator: Joachim Schirren, Prof. Dr. med.          Sub-Investigator: Servet Bölükbas, Dr. med.          Sub-Investigator: Sabine Labenz          Sub-Investigator: Birgit Wilde          Sub-Investigator: Klaudia Fischbach 收起 <<
NCT00021528 Depression Phase 4 Completed - -
NCT00080158 Depression Su... 展开 >>icide, Attempted 收起 << Phase 2 Phase 3 Completed - United States, Maryland ... 展开 >> Johns Hopkins University Baltimore, Maryland, United States, 21287 United States, New York New York University Child Study Center New York, New York, United States, 10016 Columbia University at the New York State Psychiatric Institute New York, New York, United States, 10032 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27705 United States, Pennsylvania University of Pittsburgh - Western Psychiatric Institute and Clinic Pittsburgh, Pennsylvania, United States, 15213 United States, Texas University of Texas, Southwestern Medical Center Dallas, Texas, United States, 75235 收起 <<

Mirtazapine 参考文献

[1]Garcia-Effron G, Gomez-Lopez A, et al. In vitro activity of terbinafine against medically important non-dermatophyte species of filamentous fungi. J Antimicrob Chemother. 2004 Jun;53(6):1086-9. Epub 2004 Apr 21.

[2]Anttila SA, Leinonen EV. A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64.

[3]Anttila SA, Leinonen EV. A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001;7(3):249‐264

[4]Smit M, Dolman KM, Honig A. Mirtazapine in pregnancy and lactation - A systematic review. Eur Neuropsychopharmacol. 2016;26(1):126‐135

[5]Poyurovsky M, Weizman A. Very Low-Dose Mirtazapine (7.5 mg) in Treatment of Acute Antipsychotic-Associated Akathisia. J Clin Psychopharmacol. 2018;38(6):609‐611

[6]Malamood M, Roberts A, Kataria R, Parkman HP, Schey R. Mirtazapine for symptom control in refractory gastroparesis. Drug Des Devel Ther. 2017;11:1035‐1041.

Mirtazapine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.77mL

0.75mL

0.38mL

18.84mL

3.77mL

1.88mL

37.69mL

7.54mL

3.77mL

Mirtazapine 技术信息

CAS号85650-52-8
分子式C17H19N3
分子量 265.353
别名 米氮平 ;6-Azamianserin;Org3770;Mirtazapine (CRM)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(188.43 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

动物实验配方
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