2. Neuronal Signaling GPCR/G Protein Immunology/Inflammation Protein Tyrosine Kinase/RTK Membrane Transporter/Ion Channel Apoptosis
  3. Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis
  4. Amitriptyline hydrochloride

Amitriptyline hydrochloride  (Synonyms: 盐酸阿米替林)

目录号: HY-B0527A 纯度: 99.94%
COA 产品使用指南 技术支持

Amitriptyline hydrochloride 是一种口服有效的三环类抗抑郁剂 (TCA)。Amitriptyline hydrochloride 主要通过阻断 SERT (Ki = 3.45 nM) 和 NET (Ki = 13.3 nM)，增加突触间隙中 5-羟色胺 (5-HT) 和去甲肾上腺素 (NE) 的浓度，从而发挥抗抑郁作用。Amitriptyline hydrochloride 也是 α2A 和 TrkA/TrkB 受体激动剂，从而发挥镇痛效果和神经营养活性 (抑制细胞凋亡 (apoptosis))。Amitriptyline hydrochloride 还可降低炎症、血管生成和纤维化。Amitriptyline hydrochloride 还可与 DAT (Ki = 2.58 μM) 结合。Amitriptyline hydrochloride 对一系列受体具有高亲和力，可拮抗毒蕈碱乙酰胆碱受体 (M1/M2/M3/M4/M5 受体) (Ki = 11-24 nM)、H1 受体 (Ki = 0.5-1.1 nM)、肾上腺素能 α1 受体 (Ki = 4.4 nM) 等，从而导致一系列副作用。Amitriptyline hydrochloride可阻断钠通道和 hERG 钾通道 (IC50 = 4.78 μM)，具有心脏毒性。

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Amitriptyline hydrochloride

Amitriptyline hydrochloride Chemical Structure

CAS No. : 549-18-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
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500 mg ￥500
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1 g ￥600
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5 g ￥960
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Other Forms of Amitriptyline hydrochloride:

Amitriptyline hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity[1][2][3][4][5].

IC50 & Target[1][3]

5-HT1A Receptor

450 nM (IC50)

5-HT1B Receptor

40 nM (IC50)

5-HT2A Receptor

4 nM (IC50)

5-HT2B Receptor

40 nM (IC50)

5-HT2C Receptor

6 nM (IC50)

H1 Receptor

1.1 nM (IC50)

H3 receptor

1 μM (IC50)

H4 receptor

33.6 nM (IC50)

SERT

3.45 nM (Ki)

NET

13.3 nM (Ki)

DAT

2.58 μM (Ki)

Adrenergic receptor

24 nM (IC50)

muscarinic receptor

7.2 nM (IC50)

TrkA

 

TrkB

 

体外研究
(In Vitro)

Amitriptyline hydrochloride (0.5-10 μM，3.5-16.5 小时) 可有效抵抗 T17 细胞的细胞凋亡 (EC50 = 50 nM)，且对 SN56 细胞无保护作用；在受谷氨酸刺激并经受氧糖剥夺 (OGD) 的原代大鼠海马神经元中，神经元凋亡显著减少[3]。
Amitriptyline hydrochloride (0.5 μM，30 分钟) 可诱导海马神经元中 TrkA 和 TrkB 受体的磷酸化和活化[3]。
Amitriptyline hydrochloride (0.5 μM，5 天) 可诱导 PC12 细胞的神经突生长[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Amitriptyline hydrochloride 相关抗体:

Western Blot Analysis[3]

Cell Line: Primary rat hippocampal neurons
Concentration: 0.5 μM
Incubation Time: 30 min
Result: Strongly induced phosphorylation of TrkA, TrkB, Akt, and ERK.
Induced TrkA-TrkA homodimerization, TrkB-TrkB homodimerization, and TrkA-TrkB heterodimerization.
体内研究
(In Vivo)

Amitriptyline hydrochloride (15 mg/kg，腹腔注射，每日一次，连续 5 天) 可通过激活 TrkA 和 TrkB 受体，预防小鼠脑内由 Kainic acid (HY-N2309) 诱导的神经元凋亡[3]。
Amitriptyline hydrochloride (15 mg/kg，腹腔注射，单剂量) 可通过激活小鼠中枢神经系统中的 α2A-肾上腺素能受体，在小鼠模型中产生抗伤害作用[4]。
Amitriptyline hydrochloride (5 mg/kg，口服，每日一次，连续 7 天) 能够下调植入 14 天后的血管生成和异物反应 (FBR)[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Kainic acid induced excitatory epilepsy model established in male C57BL/6 mice[3]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 5 days
Result: Effectively activated TrkA, TrkB and their downstream signaling pathways in the brain.
Significantly reduced KA-induced hippocampal (70%).
Animal Model: Hot-plate test and abdominal constriction test established in male Swiss albino mice (23-30 g)[4]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Significantly increased pain threshold in both models (increased hot plate latency and reduced writhing times).
Required the presence of endogenous monoamine neurotransmitters (such as NE).
Exhibited the analgesic effect be completely blocked by BRL 44408 (HY-12716).
Animal Model: Polyether-polyurethane sponge disks induced FBR model established in male C57BL/6 mice[5]
Dosage: 5 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
Result: Had no effect on 7-day implants.
Significantly reduced all key parameters of the 14-day implants, reducing angiogenesis, fibrosis markers, and FBR markers.
Clinical Trial
分子量

313.86

Formula

C20H24ClN
CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸阿米替林；盐酸阿密替林
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (318.61 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : ≥ 50 mg/mL (159.31 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1861 mL 15.9307 mL 31.8613 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂： PBS

    Solubility: 120 mg/mL (382.34 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.94%

COA (291 KB) HNMR (265 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

Amitriptyline hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.1861 mL 15.9307 mL 31.8613 mL 79.6534 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 mL 15.9307 mL
10 mM 0.3186 mL 1.5931 mL 3.1861 mL 7.9653 mL
15 mM 0.2124 mL 1.0620 mL 2.1241 mL 5.3102 mL
20 mM 0.1593 mL 0.7965 mL 1.5931 mL 3.9827 mL
25 mM 0.1274 mL 0.6372 mL 1.2745 mL 3.1861 mL
30 mM 0.1062 mL 0.5310 mL 1.0620 mL 2.6551 mL
40 mM 0.0797 mL 0.3983 mL 0.7965 mL 1.9913 mL
50 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5931 mL
60 mM 0.0531 mL 0.2655 mL 0.5310 mL 1.3276 mL
80 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
100 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amitriptyline549-18-8盐酸阿米替林盐酸阿密替林Serotonin Transporter5-HT ReceptormAChRHistamine ReceptorAdrenergic ReceptorTrk ReceptorSodium ChannelPotassium ChannelDopamine TransporterApoptosis5-HTTSERTSLC6A4Serotonin Receptor5-hydroxytryptamine ReceptorMuscarinic acetylcholine receptorBeta ReceptorTropomyosin related kinase receptor Na channelsNa+ channelsKcsADATSLC6A3neurotrophinsdepressionneuropathicpainneurologicpsychiatricdiseasesTrkA/TrkBheterodimerizationInhibitorinhibitorinhibit

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