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。
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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。 |
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]. |
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. |
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 |
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 | - | - |
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 |
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 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
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