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> Amitriptyline (hydrochloride) [549-18-8]

Amitriptyline (hydrochloride) [549-18-8]

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Cat# HY-B0527A-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.

For research use only. We do not sell to patients.

Amitriptyline hydrochloride Chemical Structure

Amitriptyline hydrochloride Chemical Structure

CAS No. : 549-18-8

This product is a controlled substance and not for sale in your territory.

Based on 3 publication(s) in Google Scholar

Other Forms of Amitriptyline hydrochloride:

  • Amitriptyline-d3 hydrochloride In-stock
  • Amitriptyline In-stock
  • Amitriptyline-d6 hydrochloride In-stock
  • Amitriptyline hydrochloride (Standard) Get quote

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View All Adrenergic Receptor Isoform Specific Products:

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Description

Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].

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

 

In Vitro

Amitriptyline hydrochloride (30 min) protects hippocampal neurons (T17 cells) from apoptosis (EC50: 50 nM)[3].
Amitriptyline hydrochloride (0.5 μM, 30 min) induces TrkA and TrkB receptor phosphorylation and activation in hippocampal neurons[3].
Amitriptyline hydrochloride (500 nM, 5 days) induces neurite outgrowth in PC12 cells[3].

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

Amitriptyline hydrochloride Related Antibodies

Western Blot Analysis[3]

Cell Line: hippocampal neurons
Concentration: 0.5 μM
Incubation Time: 30 min
Result: Induced TrkA phosphorylation.
Induced Erk 1/2 and Akt signalings activation.
In Vivo

Amitriptyline (15 mg/kg, i.p.) hydrochloride activates TrkA and TrkB receptors, and prevents Kainic acid (HY-N2309)-induced neuronal apoptosis in brain of C57BL/6 mice[3].
Amitriptyline (15-25 mg/kg, i.p., 5 days) hydrochloride induces TrkA and TrkB hetero-dimerization in mouse brain[3].
Amitriptyline (15 mg/kg, i.p.) hydrochloride shows antinociceptive effect by activation of α2-adrenoceptors in mice[3].

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

Animal Model: Mice[2]
Dosage: 15-25 mg/kg
Administration: i.p., 5 days
Result: Induces TrkA tyrosine phosphorylation.
Induces TrkA and TrkB receptor heterodimerization in the brain.
Clinical Trial
Molecular Weight

313.86

Formula

C20H24ClN
CAS No.

549-18-8
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (318.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (159.31 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 120 mg/mL (382.34 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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

    [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.  [Content Brief]

    [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.  [Content Brief]

    [4]. Ghelardini C, et al. Antinociception induced by amitriptyline and imipramine is mediated by alpha2A-adrenoceptors. Jpn J Pharmacol. 2000 Feb;82(2):130-7.  [Content Brief]

  • [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.

    [4]. Ghelardini C, et al. Antinociception induced by amitriptyline and imipramine is mediated by alpha2A-adrenoceptors. Jpn J Pharmacol. 2000 Feb;82(2):130-7.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Amitriptyline hydrochloride Related Classifications

Help & FAQs

Keywords:

Amitriptyline549-18-8Serotonin Transporter5-HT ReceptorHistamine ReceptormAChRAdrenergic ReceptorSodium ChannelTrk Receptor5-HTTSERTSLC6A4Serotonin Receptor5-hydroxytryptamine ReceptorMuscarinic acetylcholine receptorBeta ReceptorNa channelsNa+ channelsTropomyosin related kinase receptorneurotrophinsdepressionneuropathicpainneurologicpsychiatricdiseasesTrkA/TrkBheterodimerizationInhibitorinhibitorinhibit

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