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

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

Imipramine HCl 是一种三环类抗抑郁药,抑制血清素和去甲肾上腺素转运蛋白,Ki 值分别为 7.7 nM 和 67 nM。

Imipramine HCl/盐酸丙咪嗪 化学结构 CAS号:113-52-0
Imipramine HCl/盐酸丙咪嗪 化学结构
CAS号:113-52-0
Imipramine HCl/盐酸丙咪嗪 3D分子结构
CAS号:113-52-0
Imipramine HCl/盐酸丙咪嗪 化学结构 CAS号:113-52-0
Imipramine HCl/盐酸丙咪嗪 3D分子结构 CAS号:113-52-0
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Imipramine HCl/盐酸丙咪嗪 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]}
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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 99%
Fluvoxamine maleate 99%
Iloperidone 99%
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 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 99%
Fluoxetine HCl 99.5%
Paroxetine HCl AChR 99%
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

95%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

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

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

98%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 99%
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%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

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

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

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-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

95%
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 HCl/盐酸丙咪嗪 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 HCl/盐酸丙咪嗪 细胞实验

Cell Line
Concentration Treated Time Description References
TgF344-AD rat primary neurons 1 μM 14 days Evaluate the effect of Imipramine on pTau neuropathology, results showed Imipramine significantly reduced pTau neuropathology Alzheimers Res Ther. 2022 Jun 29;14(1):88.
5xFAD mouse primary neurons 0.01, 0.1, 1.0 μM 9 days Evaluate the effect of Imipramine on Aβ neuropathology, results showed Imipramine significantly reduced Aβ neuropathology Alzheimers Res Ther. 2022 Jun 29;14(1):88.
Primary astrocytes 10 µM 24 h Attenuated microglia-conditioned medium-induced astrocyte activation (GFAP/C3b downregulation) and ceramide (Cer) generation Acta Neuropathol Commun. 2023 Aug 21;11(1):135.
Primary microglia 10 µM 18 h Inhibited Aβ oligomer-induced acid sphingomyelinase (A-SMase) activity and reduced proinflammatory cytokine (C1q, TNF-α, IL-1α) release Acta Neuropathol Commun. 2023 Aug 21;11(1):135.
colon epithelial Caco-2 cells 120 mg/L 30 and 90 min Evaluate IMI's effect on Zn permeability; results showed enhanced Zn transcellular transport Nutrients. 2020 Aug 20;12(9):2529.
bovine ventricular muscle 0.01 μM to 50 μM 30 min To study the effects of imipramine on action potential characteristics in bovine ventricular muscle. Results showed that imipramine at concentrations higher than 5 μM significantly decreased action potential amplitude, overshoot, and Vmax without affecting the resting membrane potential. Additionally, imipramine shortened both the action potential duration (APD) and the effective refractory period (ERP). Br J Pharmacol. 1980 Sep;70(1):15-23.
bovine Purkinje fibres 0.01 μM to 50 μM 30 min To study the effects of imipramine on action potential characteristics in bovine Purkinje fibres. Results showed that imipramine at concentrations higher than 1 μM significantly decreased action potential amplitude, overshoot, and maximum rate of depolarization (Vmax) without affecting the resting membrane potential. Additionally, imipramine decreased conduction velocity and altered membrane responsiveness and recovery time curves. Br J Pharmacol. 1980 Sep;70(1):15-23.

Imipramine HCl/盐酸丙咪嗪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Repeated Social Defeat (RSD) model Drinking water administration 15mg/kg Daily administration for 6 days Imipramine diminished stress-induced inflammation in the periphery and central nervous system and related anxiety- and depressive- like behaviors. Brain Behav Immun. 2016 Oct;57:293-303
Female Lister hooded rats Y-maze exploratory activity model Intraperitoneal injection 10 mg/kg (first 3 days) and 2.5 mg/kg (4th day) Once daily for 3 consecutive days, once on the 4th day Imipramine pretreatment abolished naturally-occurring and drug-induced differences in exploratory activity, making rat behavior more uniform. Br J Pharmacol. 1980 Oct;70(2):277-85
Rats Wistar rats Subcutaneous injection 5 mg/kg Once daily for 28 days To investigate the effects of long-term imipramine treatment on m-CPP-induced suppression of locomotor activity and food intake. Results showed that long-term imipramine treatment enhanced the locomotor and food intake suppressant effects of m-CPP. Br J Pharmacol. 1987 Aug;91(4):747-52
5xFAD transgenic mice (Alzheimer’s disease model) Alzheimer’s disease model Intraperitoneal injection 15 µg/g Once daily for 28 days Reduced microglial/astrocytic activation, decreased GFAP/Cer/Aβ levels in brain-derived EVs, improved mitochondrial dysfunction, and ameliorated AD pathology (e.g., plaque deposition and neuronal death) Acta Neuropathol Commun. 2023 Aug 21;11(1):135.
Sprague-Dawley rats Pilocarpine-induced seizure model Intraperitoneal injection 10 mg/kg Once weekly for four weeks To evaluate the effects of imipramine on neuronal survival, oxidative stress, apoptosis, and cognitive function after seizures. Results showed that four weeks of imipramine treatment significantly increased hippocampal neuron survival, reduced oxidative stress marker 4HNE levels, decreased the Bax/Bcl-2 ratio, and improved spatial cognitive function. Cells. 2025 Feb 14;14(4):281
Sprague-Dawley rats Severe hypoglycemia model Intraperitoneal injection 10 mg/kg Once per day for 7 days To investigate the protective effects of imipramine on hypoglycemia-induced neuronal death. Results showed that imipramine significantly reduced hypoglycemia-induced hippocampal neuronal death and improved cognitive function. Cells. 2022 Feb 14;11(4):667
Wistar rats Bipolar disorder model Intraperitoneal injection 10 mg/kg Once daily for 5 days To investigate the effect of IMI administration in rats submitted to OUA-induced bipolar disorder model. Results showed that IMI elicited significant mania switch-like effect in OUA-treated animals. J Affect Disord. 2022 Feb 15;299:425-434
Male Albino Swiss mice Forced swim test (FST) depression model Oral (p.o.) 60 mg/kg Single dose, 60 min before testing Evaluate antidepressant efficacy and Zn redistribution; results demonstrated synergistic increase in brain Zn levels and BDNF/pCREB Nutrients. 2020 Aug 20;12(9):2529.
Rat Rat caudate putamen Oral 10 mg/kg Twice a day for 14 days To investigate the effect of prolonged imipramine treatment on the level of mRNA coding for D2 dopamine receptors in the rat caudate putamen, showing that repeated administration resulted in a significant increase in D2 dopamine receptor mRNA levels. Br J Pharmacol. 1998 Mar;123(5):833-8

Imipramine HCl/盐酸丙咪嗪 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 HCl/盐酸丙咪嗪 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 HCl/盐酸丙咪嗪 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 HCl/盐酸丙咪嗪 技术信息

CAS号113-52-0
分子式C19H25ClN2
分子量 316.87
SMILES Code CN(C)CCCN1C2=CC=CC=C2CCC3=CC=CC=C31.[H]Cl
MDL No. MFCD00012669
别名 丙咪嗪盐酸盐 ;Imipramine (hydrochloride); Imipramine HCl; Melipramine
运输蓝冰
InChI Key XZZXIYZZBJDEEP-UHFFFAOYSA-N
Pubchem ID 8228
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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