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/ Amitriptyline HCl

阿米替林盐酸盐 /Amitriptyline HCl {[allProObj[0].p_purity_real_show]}

货号：A315453 同义名： 盐酸阿米替林 / Amitriptyline (hydrochloride) (CRM);Ro 4-1517

Amitriptyline HCl is a multiple-target molecular as an inhibitor of both 5-HT and NA reuptake (SNRI), and also a TrkA/B agonist.

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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Amitriptyline HCl 化学结构 CAS号：549-18-8
Amitriptyline HCl 化学结构
CAS号：549-18-8
Amitriptyline HCl 3D分子结构
CAS号：549-18-8
Amitriptyline HCl 化学结构 CAS号：549-18-8
Amitriptyline HCl 3D分子结构 CAS号：549-18-8
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Amitriptyline HCl 纯度/质量文件 产品仅供科研

货号：A315453 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
• JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]
• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
• J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]
• PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]
更多 >
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。

Amitriptyline HCl 生物活性

描述 Amitriptyline hydrochloride acts as an inhibitor of the serotonin reuptake transporter (SERT) and the noradrenaline reuptake transporter (NET), with inhibition constants (Kis) of 3.45 nM for SERT and 13.3 nM for NET in humans. Additionally, it has a low affinity for the dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also blocks adrenergic, muscarinic, histamine, and 5-HT receptors. It serves as an agonist for TrkA and TrkB receptors, demonstrating strong neurotrophic properties. Amitriptyline hydrochloride is recognized for its antidepressant efficacy[1].[2].[3].
体内研究

Amitriptyline (15 mg/kg, i.p.) hydrochloride stimulates TrkA and TrkB receptors and obstructs neuronal apoptosis induced by Kainic acid in the brains of C57BL/6 mice[3].

Amitriptyline (15-25 mg/kg, i.p., over 5 days) hydrochloride causes TrkA and TrkB receptors to form heterodimers in the mouse brain[3].

Amitriptyline (15 mg/kg, i.p.) hydrochloride demonstrates an antinociceptive action by activating α2-adrenoceptors in mice[3].
体外研究

Amitriptyline hydrochloride (30 min exposure) safeguards hippocampal neurons (T17 cells) against apoptosis with an EC50 of 50 nM[3].

Amitriptyline hydrochloride (0.5 μM, 30 min) prompts phosphorylation and activation of TrkA and TrkB receptors in hippocampal neurons[3].

Amitriptyline hydrochloride (500 nM, over 5 days) promotes neurite extension in PC12 cells[3].

Amitriptyline HCl 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
NCT03168022 Healthy Adults Phase 1 Completed - Canada ... 展开 >> InVentiv Health Clinique Inc. Quebec, Canada, GIP )A2 收起 <<
NCT02814565 Neck Pain Bac... 展开 >>k Pain Spasm 收起 << Phase 3 Completed - Russian Federation ... 展开 >> Lipetsk, Lipetsk region, Russian Federation Saransk, Republic of Mordovia, Russian Federation Kazan, Republic of Tatarstan, Russian Federation Ekaterinburg, Sverdlovsk region, Russian Federation Moscow, Russian Federation Nizhny Novgorod, Russian Federation Novosibirsk, Russian Federation Saint-Petersburg, Russian Federation Tver, Russian Federation Yaroslavl, Russian Federation 收起 <<
NCT01266733 Fibromyalgia Phase 2 Completed - Spain ... 展开 >> Hospital Galdakao-Usansolo Galdakao, Bizkaia, Spain, 48960 收起 <<

Amitriptyline HCl 参考文献

[1]Kim Lawson. A Brief Review of the Pharmacology of Amitriptyline and Clinical Outcomes in Treating Fibromyalgia. Biomedicines. 2017 Jun; 5(2): 24.

[2]S Neil Vaishnavi , et al. Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1;55(3):320-2.

[3]Jang, S.W., et al., Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol, 2009. 16(6): p. 644-56.

Amitriptyline HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.19mL

0.64mL

0.32mL

15.93mL

3.19mL

1.59mL

31.86mL

6.37mL

3.19mL

Amitriptyline HCl 技术信息

CAS号549-18-8
分子式C20H24ClN
分子量 313.864
别名 盐酸阿米替林 ;Amitriptyline (hydrochloride) (CRM);Ro 4-1517;NIH 10794;Amitriptyline hydrochloride
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(334.54 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: 50 mg/mL(159.3 mM)
动物实验配方

Tags: Amitriptyline | 549-18-8 | Serotonin Transporter Inhibitor | Neuronal Signaling | GPCR/G Protein | Immunology/Inflammation | Membrane Transporter/Ion Channel | Protein Tyrosine Kinase/RTK | Serotonin Transporter | 5-HT Receptor | Histamine Receptor | mAChR | Adrenergic Receptor | Sodium Channel | Trk Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Amitriptyline HCl 纯度/质量文件 | Amitriptyline HCl 亚型比较 | Amitriptyline HCl 生物活性 | Amitriptyline HCl 临床数据 | Amitriptyline HCl 参考文献 | Amitriptyline HCl 实验方案 | Amitriptyline HCl 技术信息

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