Art. -Nr.: HY-B0527

Amitriptyline

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

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

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Reinheit: 99.93%
CAS. Nr.: 50-48-6
Formel: C₂₀H₂₃N
Molecular Weight:277.40

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Amitriptyline Chemical Structure

CAS. Nr.: 50-48-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[3]

TrkA

TrkB

5-HT Receptor

Histamine Receptor

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle mAChR Isoform-spezifische Produkte anzeigen :

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	3 μM Compound: Amitryptline	Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole-cell patch clamp assay Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole-cell patch clamp assay	[PMID: 30653317]
CHO-K1	IC₅₀	1.6 μM Compound: amitriptyline	Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay Inhibition of human NaV1.5 alpha subunit expressed in CHOK1 cells at -90 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
CHO-K1	IC₅₀	3.1 μM Compound: amitriptyline	Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay Inhibition of human NaV1.2 alpha subunit expressed in CHOK1 cells at -65 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	16.9 μM Compound: amitriptyline	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
HEK293	IC₅₀	1 μM Compound: amitriptyline	Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	12 μM Compound: amitriptyline	Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay Inhibition of human NaV1.7 F1737A mutant expressed in HEK293 cells at -65 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	7 μM Compound: amitriptyline	Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay Inhibition of recombinant human NaV1.7 alpha subunit expressed in HEK293 cells at -90 mV holding potential by patch clamp electrophysiological assay	[PMID: 22770500]
HEK293	IC₅₀	9.6 μM Compound: Amitriptyline	Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting method Inhibition of [3H]-dofetilide binding to human ERG expressed in HEK293 cell membranes measured after 1 hr by liquid scintillation counting method	[PMID: 30597328]
HepG2	IC₅₀	29.6 μM Compound: Amitriptyline	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis	[PMID: 32442850]
NCI-H1650	GI₅₀	>40 μM Compound: Amitriptyline	Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 26372073]
SH-SY5Y	IC₅₀	48.1 μM Compound: Amitriptyline	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability by measuring ATP content incubated for 24 hrs by luminescent analysis	[PMID: 32442850]

In Vitro

Amitriptyline (0.5-10 μM, 3.5-16.5 h) effectively resists cell apotosis (EC₅₀ = 50 nM) in T17 cells and shows no protective effect on the SN56 cells, and in primary rat hippocampal neurons stimulated by glutamate and subjected to oxygen-glucose deprivation (OGD), the neuronal apoptosis is significantly reduced^[3].
Amitriptyline (0.5 μM, 30 min) induces TrkA and TrkB receptor phosphorylation and activation in hippocampal neurons^[3].
Amitriptyline (0.5 μM, 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.

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.

In Vivo

Amitriptyline (15 mg/kg, i.p., once daily for 5 days) prevents Kainic acid (HY-N2309)-induced neuronal apoptosis in mice brain by activating TrkA and TrkB receptors^[3].
Amitriptyline (15 mg/kg, i.p., single dose) produces antinociception in a mouse model by activating α2A-adrenoceptor receptors in the central nervous system^[4].
Amitriptyline (5 mg/kg, p.o., once daily for 7 days) is able to down-regulate angiogenesis and foreign body reaction (FBR) in 14-day-old implants^[5].

MedChemExpress (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.

Chemical Information

CAS. Nr. 50-48-6
Appearance Liquid (Density: 1.076±0.06 g/cm³)
Molecular Weight 277.40
Formel C₂₀H₂₃N
Color Colorless to light yellow
SMILES

CN(CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (8)

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Journal Impact Factor

J Am Chem Soc

Fluorinated Ribonucleocarbohydrate Nanoparticles Allow Ultraefficient mRNA Delivery and Protein Expression in Tumor-Associated Myeloid Cells. [Abstract]

2025 Mar 26. PMID: 40135499
NPJ Digit Med

Tandospirone augments cisplatin treatment by lowering cholesterol and managing distress in NSCLC patients. [Abstract]

2025 Nov 17;8(1):663. PMID: 41249389
Cell Commun Signal

Tricyclic antidepressants induce liver inflammation by targeting NLRP3 inflammasome activation. [Abstract]

2023 May 25;21(1):123. PMID: 37231437
Neurosci Bull

Electrophysiological Abnormalities and Pharmacological Corrections of Pathogenic Missense Variants in KCNQ3. [Abstract]

2025 Mar 17. PMID: 40095209
Int Immunopharmacol

Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy. [Abstract]

2025 Jan 6:147:113969. PMID: 39764996
J Med Virol

Irradiation accelerates SARS-CoV-2 infection by enhancing sphingolipid metabolism. [Abstract]

2023 Jan;95(1):e28266. PMID: 36319186
Skelet Muscle

ASM is a therapeutic target in dermatomyositis by regulating the differentiation of naive CD4 + T cells into Th17 and Treg subsets. [Abstract]

2024 Jul 18;14(1):16. PMID: 39026344
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (360.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6049 mL

18.0245 mL

36.0490 mL

5 mM

0.7210 mL

3.6049 mL

7.2098 mL

10 mM

0.3605 mL

1.8025 mL

3.6049 mL

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (952 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[5]. Scheuermann K, et al. Amitriptyline efficacy in decreasing implant-induced foreign body reaction. IUBMB Life. 2023 Sep;75(9):732-742. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6049 mL	18.0245 mL	36.0490 mL	90.1226 mL
	5 mM	0.7210 mL	3.6049 mL	7.2098 mL	18.0245 mL
	10 mM	0.3605 mL	1.8025 mL	3.6049 mL	9.0123 mL
	15 mM	0.2403 mL	1.2016 mL	2.4033 mL	6.0082 mL
	20 mM	0.1802 mL	0.9012 mL	1.8025 mL	4.5061 mL
	25 mM	0.1442 mL	0.7210 mL	1.4420 mL	3.6049 mL
	30 mM	0.1202 mL	0.6008 mL	1.2016 mL	3.0041 mL
	40 mM	0.0901 mL	0.4506 mL	0.9012 mL	2.2531 mL
	50 mM	0.0721 mL	0.3605 mL	0.7210 mL	1.8025 mL
	60 mM	0.0601 mL	0.3004 mL	0.6008 mL	1.5020 mL
	80 mM	0.0451 mL	0.2253 mL	0.4506 mL	1.1265 mL
	100 mM	0.0360 mL	0.1802 mL	0.3605 mL	0.9012 mL

Amitriptyline

8 Cited Publications

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Amitriptyline

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Publications Citing Use of MedChemExpress (MCE) Amitriptyline

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle mAChR Isoform-spezifische Produkte anzeigen

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Amitriptyline Related Classifications

Art. -Nr.: HY-B0527