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Amitriptyline (hydrochloride)

CAT: 0804-HY-B0527A-01Size: 5 gDry Ice: NoHazardous: No
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CAT#:0804-HY-B0527A-01Size:5 g
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
549-18-8
UNSPSC
12352005
Hazard Statement
H301
Target
5-HT Receptor; Adrenergic Receptor; Apoptosis; Dopamine Transporter; Histamine Receptor; mAChR; Potassium Channel; Serotonin Transporter; Sodium Channel; Trk Receptor
Type
Reference compound
Related Pathways
Apoptosis; GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling; Protein Tyrosine Kinase/RTK
Applications
Neuroscience-Neurodegeneration
Field of Research
Endocrinology; Inflammation/Immunology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/amitriptyline-hydrochloride.html
Concentration
10mM
Purity
99.94
Solubility
DMSO : ≥ 100 mg/mL|H2O : ≥ 50 mg/mL
Smiles
CN(C)CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3.Cl
Molecular Formula
C20H24ClN
Molecular Weight
313.86
Precautions
H301
References & Citations
[1]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.|[2]Kim Lawson. A Brief Review of the Pharmacology of Amitriptyline and Clinical Outcomes in Treating Fibromyalgia. Biomedicines. 2017 Jun; 5 (2) : 24.|[3]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.|[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. |[5]Scheuermann K, et al. Amitriptyline efficacy in decreasing implant-induced foreign body reaction. IUBMB Life. 2023 Sep;75 (9) :732-742.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
H1 Receptor; H3 Receptor; H4 Receptor; mLAG-3; TrkA; TrkB; α-1 microglobulin
Citation 01
Cell Commun Signal. 2023 May 25;21 (1) :123.|J Med Virol. 2023 Jan;95 (1) :e28266.|PLoS Negl Trop Dis. 2019 Aug 20;13 (8) :e0007681. |Skelet Muscle. 2024 Jul 18;14 (1) :16.|Int Immunopharmacol. 2025 Jan 6:147:113969.|J Am Chem Soc. 2025 Apr 9;147 (14) :11766-11776.|Neurosci Bull. 2025 Mar 17.|NPJ Digit Med. 2025 Nov 17;8 (1) :663.

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