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Amitriptyline HCl

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Chemical Structure| 549-18-8 同义名 : 盐酸阿米替林 ;Amitriptyline (hydrochloride) (CRM);Ro 4-1517;NIH 10794;Amitriptyline hydrochloride
CAS号 : 549-18-8
货号 : A315453
分子式 : C20H24ClN
纯度 : 98%
分子量 : 313.864
MDL号 : MFCD00012537
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 <<
实验方案
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
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.