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5-羟色胺受体
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/ Imipramine hydrochloride

盐酸丙咪嗪 /Imipramine hydrochloride {[allProObj[0].p_purity_real_show]}

货号：A131108 同义名： 丙咪嗪盐酸盐 / Imipramine (hydrochloride);Imipramine HCl

Imipramine HCl is a tricyclic inhibitor of both serotonin and norepinephrine transporters with Ki values of 7.7 nM and 67 nM, respectively.

Imipramine hydrochloride 化学结构 CAS号：113-52-0
Imipramine hydrochloride 化学结构
CAS号：113-52-0
Imipramine hydrochloride 3D分子结构
CAS号：113-52-0
Imipramine hydrochloride 化学结构 CAS号：113-52-0
Imipramine hydrochloride 3D分子结构 CAS号：113-52-0
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Imipramine hydrochloride 纯度/质量文件 产品仅供科研

货号：A131108 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

Imipramine hydrochloride 生物活性

描述 Imipramine HCl inhibits serotonin transporter with an IC50 value of 32 nM in vitro[2]. Imipramine (IMI) reduces pain-related negative emotion without influencing pain and that this effect is diminished by denervation of 5-HT neurons and by anti-BDNF (brain-derived neurotrophic factor) treatment. IMI also normalizes derangement of ERK/CREB coupling, which leads to induction of BDNF[3]. Moreover, imipramine treatment counteracts the corticosterone-induced increase in the reactivity of the hippocampal circuitry to the activation of the 5-HT7 receptor[1]. Administration of imipramine reverses social avoidance behavior, significantly increasing the interaction time. 24 days of imipramine treatment in RSD (repeated social defeat) mice significantly decreases stress-induced mRNA levels for IL-6 in brain microglia[4]. Chronic mild stress induces a long-term altered gene expression profile in the prefrontal cortex that is partially reverted by imipramine treatment (10 mg/kg, i.p.)[5]. Chronic imipramine administration altered the amino acid dynamics in the brain. In the striatum, the concentrations of asparagine, glutamine and methionine were significantly increased by chronic imipramine administration. In the thalamus and hypothalamus, chronic imipramine administration significantly decreased the valine concentration. In addition, lower concentration of asparagine in the prefrontal cortex of WKY rats (Wistar Kyoto rats, an animal model of depression) was improved by chronic imipramine administration[6].

Imipramine 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
NCT02191358 - Completed - United States, California ... 展开 >> Dr. Michael Dao Garden Grove, California, United States, 92844 United States, Colorado Kaiser Permanente Colorado Denver, Colorado, United States, 80011 United States, Kentucky Gill Heart Institute Lexington, Kentucky, United States, 40508 United States, Maryland IRC Clinics Towson, Maryland, United States, 21204 United States, Massachusetts Internal Medicine & Cardiology Associates Fall River, Massachusetts, United States, 02720 Prima CARE Fall River, Massachusetts, United States, 02720 United States, Virginia Carilion Clinic Christiansburg, Virginia, United States, 24073 收起 <<
NCT00000464 Arrhythmia Ca... 展开 >>rdiovascular Diseases Heart Arrest Heart Diseases Myocardial Infarction Ventricular Fibrillation 收起 << Phase 3 Completed - -
NCT00000518 Arrhythmia Ca... 展开 >>rdiovascular Diseases Death, Sudden, Cardiac Heart Diseases Tachycardia, Ventricular Ventricular Arrhythmia Ventricular Fibrillation 收起 << Phase 3 Completed - -

Imipramine hydrochloride 参考文献

[1]Tokarski K, Pitra P, Duszynska B, Hess G. Imipramine counteracts corticosterone-induced alterations in the effects of the activation of 5-HT(7) receptors in rat hippocampus. J Physiol Pharmacol. 2009;60(2):83‐88

[2]Balkovetz DF, Tiruppathi C, Leibach FH, Mahesh VB, Ganapathy V. Evidence for an imipramine-sensitive serotonin transporter in human placental brush-border membranes. J Biol Chem. 1989;264(4):2195‐2198

[3]Yasuda S, Yoshida M, Yamagata H, et al. Imipramine ameliorates pain-related negative emotion via induction of brain-derived neurotrophic factor. Cell Mol Neurobiol. 2014;34(8):1199‐1208

[4]Ramirez K, Shea DT, McKim DB, Reader BF, Sheridan JF. Imipramine attenuates neuroinflammatory signaling and reverses stress-induced social avoidance. Brain Behav Immun. 2015;46:212‐220

[5]Erburu M, Cajaleon L, Guruceaga E, et al. Chronic mild stress and imipramine treatment elicit opposite changes in behavior and in gene expression in the mouse prefrontal cortex. Pharmacol Biochem Behav. 2015;135:227‐236

[6]Nagasawa M, Otsuka T, Yasuo S, Furuse M. Chronic imipramine treatment differentially alters the brain and plasma amino acid metabolism in Wistar and Wistar Kyoto rats. Eur J Pharmacol. 2015;762:127‐135

Imipramine hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.78mL

3.16mL

1.58mL

31.56mL

6.31mL

3.16mL

Imipramine hydrochloride 技术信息

CAS号113-52-0
分子式C19H25ClN2
分子量 316.868
别名 丙咪嗪盐酸盐 ;Imipramine (hydrochloride);Imipramine HCl;Melipramine
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 105 mg/mL(331.37 mM)，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: 60 mg/mL(189.35 mM)，配合低频超声助溶
动物实验配方

Tags: Imipramine hydrochloride | Imipramine (hydrochloride);Imipramine HCl;Melipramine | 丙咪嗪盐酸盐 | 5-HT Receptor | SERT | AmBeed-信号通路专用抑制剂 | Imipramine hydrochloride 纯度/质量文件 | Imipramine hydrochloride 亚型比较 | Imipramine hydrochloride 生物活性 | Imipramine hydrochloride 临床数据 | Imipramine hydrochloride 参考文献 | Imipramine hydrochloride 实验方案 | Imipramine hydrochloride 技术信息

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