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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 (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 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 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 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, pIC50: 10.4 5-HT2B, pKi: 9.5 |
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-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 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-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 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-HT1B, pKi: 6.1 5-HT1D, pKi: 6 |
++
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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |