Amitriptyline hydrochloride
Based on 8 publication(s) in Google Scholar
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.
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- Pureté: 99.94%
- CAS No.: 549-18-8
- Formule: C20H24ClN
- Masse moléculaire:313.86
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Amitriptyline hydrochloride
More- J Am Chem Soc. 2025 Mar 26. [Abstract]
- NPJ Digit Med. 2025 Nov 17;8(1):663. [Abstract]
- Cell Commun Signal. 2023 May 25;21(1):123. [Abstract]
- Neurosci Bull. 2025 Mar 17. [Abstract]
- Int Immunopharmacol. 2025 Jan 6:147:113969. [Abstract]
- J Med Virol. 2023 Jan;95(1):e28266. [Abstract]
- Skelet Muscle. 2024 Jul 18;14(1):16. [Abstract]
- PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]
Voir tous les produits spécifiques à Isoform 5-HT Receptor
MoreVoir tous les produits spécifiques à Isoform Histamine Receptor
MoreVoir tous les produits spécifiques à Isoform Adrenergic Receptor
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Activité biologique
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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 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.2 μM
Compound: Amitriptyline
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Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
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[PMID: 34112854] |
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.
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Cell Line:Primary rat hippocampal neurons
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Concentration:0.5 μM
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Incubation Time:30 min
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Result:Strongly induced phosphorylation of TrkA, TrkB, Akt, and ERK.
Induced TrkA-TrkA homodimerization, TrkB-TrkB homodimerization, and TrkA-TrkB heterodimerization.
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.
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Animal Model:Kainic acid induced excitatory epilepsy model established in male C57BL/6 mice[3]
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Dosage:15 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 5 days
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Result:Effectively activated TrkA, TrkB and their downstream signaling pathways in the brain. Significantly reduced KA-induced hippocampal (70%).
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Animal Model:Hot-plate test and abdominal constriction test established in male Swiss albino mice (23-30 g)[4]
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Dosage:15 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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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).
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Animal Model:Polyether-polyurethane sponge disks induced FBR model established in male C57BL/6 mice[5]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), once daily for 7 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 549-18-8
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Appearance Solid
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Masse moléculaire 313.86
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Formule C20H24ClN
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Color White to off-white
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SMILES
CN(C)CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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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
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
Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 120 mg/mL (382.34 mM); Clear solution; Need ultrasonic
Pureté et documentation
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Fiche technique (286 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
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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