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 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.

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

Amitriptyline hydrochloride

Amitriptyline hydrochloride Chemical Structure

CAS No. : 549-18-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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5 g In-stock
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Based on 7 publication(s) in Google Scholar

Other Forms of Amitriptyline hydrochloride:

Amitriptyline hydrochloride Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

In Vitro

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

Amitriptyline hydrochloride Related Antibodies

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 hydrochloride (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 hydrochloride (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 hydrochloride (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.
Clinical Trial
Molecular Weight

313.86

Formula

C20H24ClN
CAS No.
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
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Concentration
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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

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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

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(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

Purity: 99.94%

SDS (480 KB)

COA (253 KB) HNMR (265 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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
  • 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:

Amitriptyline549-18-8Serotonin 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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