Amitriptyline hydrochloride

SKU: orb1310394

Description

Amitriptyline hydrochloride is a tricyclic dibenzocycloheptadiene derivative used as an antidepressant in research. It is widely applied in neuroscience studies for investigating mechanisms of chronic pain, depression, and neuropathic conditions in both in vitro and in vivo models.

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 549-18-8
• MW: 313.86
• Purity: 97.00%
• Formula: C₂₀H₂₄ClN
• SMILES: Cl.CN(C)CC\C=C1\c2ccccc2CCc2ccccc12
• Target: Norepinephrine,Sodium Channel,Adrenergic Receptor,Histamine Receptor,Sigma receptor,5-HT Receptor,Apoptosis,Serotonin Transporter,Dopamine Receptor,Potassium Channel,AChR,Trk receptor
• Solubility: Ethanol:59 mg/mL (187.98 mM);DMSO:250 mg/mL (796.53 mM);H2O:12 mg/mL (38.23 mM)

Bioactivity

• Target IC50:
  5-HT receptor:3.45 nM|5-HT2B receptor:40 nM|DAT:2.58 μM (Ki)|σ1 receptor:287 nM|H4 receptor:33.6 nM|H3 receptor:1 μM|Norepinephrine receptor:13.3 nM|5-HT2C receptor:6 nM|5-HT4:7.31 nM|mAChR:7.2 nM|5-HT2:235 nM|H1 Receptor:1.1 nM|5-HT1A receptor:450 nM|Adrenoceptor:24 nM|5-HT1B receptor:40 nM|5-HT2A receptor:4 nM
• In Vivo:
  Amitriptyline (15 mg/kg, i.p.) activates TrkA and TrkB receptors and significantly reduces kainic acid-triggered neuronal cell death in mice. Amitriptyline (15 mg/kg and 30 mg/kg, i.p.) dose-dependently decreases the immobility time in the forced swimming test (FST) of mice. Amitriptyline (15 mg/kg, i.p.) shows a significant 24-h rhythm in the immobility time in the forced swimming test (FST) of mice. Amitriptyline (1 mg/kg and 3 mg/kg) significantly increases the total distance travelled of mice in novel cages. Amitriptyline (10 mg/kg p.o., twice daily) considerably attenuates the hypothermic response to 8-OHDPAT and mCPP in mice. Amitriptyline (10 mg/kg p.o., twice daily) significantly reduces serotonin transporter density by approximately 20% in cortex of mice.
• In Vitro:
  Amitriptyline inhibits Forskolin-stimulated cyclic AMP accumulation with EC50 values of 16.2 μM in intact CHO/DOR cells. Amitriptyline causes a concentration-dependent stimulation of ERK1/2 and GSK-3β phosphorylation with EC50 values of 9.0 μM in CHO/DOR cells. Amitriptyline (15 μM) causes a stimulation of ERK1/2 phosphorylation in C6 cells. Amitriptyline (30 μM) inhibits Forskolin-stimulated adenylyl cyclase activity and antagonizes ( )-U50,488 inhibitory effect in rat nucleus accumbens. Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization. Amitriptyline (< 500 nM) promotes TrkA autophosphorylation in primary neurons and induces neurite outgrowth in PC12 cells. Amitriptyline selectively protects T17 cells from apoptosis with EC50 of 50 nM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

σ1, Tryptizol, Tropomyosin related kinase receptor, Trk Receptor, Trk receptor, TrkA/TrkB, Trkreceptor, Sodium Channel, SodiumChannel, SLC6A4, psychiatric, SerotoninTransporter, Serotonin Transporter, Serotonin Receptor, SERT, Sigmareceptor, Sigma receptor, heterodimerization, HistamineReceptor, Histamine Receptor, Muscarinic acetylcholine receptor, Norepinephrine receptor, inhibit, Inhibitor, mAChR, pain, Na+ channels, Na channels, neurotrophins, neuropathic, neurologic, 5-HT, 5-HT4, 5-HTT, 5HTReceptor, 5-hydroxytryptamine Receptor, Adrenergic Receptor, AdrenergicReceptor, 5-HT2, 5-HT Receptor, 5HT Receptor, Amitriptyline HCl, Amitriptyline Hydrochloride, Amitriptyline hydrochloride, Amitriptyline, Annoyltin, depression, Domical, diseases, Beta Receptor

Compound Identifiers

PubChem CID

11065