| Name | Amitriptyline hydrochloride |
| Description | Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities. |
| 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. [5] 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. [6] |
| In vivo | Amitriptyline (15 mg/kg, i.p.) activates TrkA and TrkB receptors and significantly reduces kainic acid-triggered neuronal cell death in mice. [6] 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. [7] 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. [8] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (159.31 mM), Sonication is recommended.
H2O : 12 mg/mL (38.2 mM)
Ethanol : 59 mg/mL (188 mM)
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| Keywords | Serotonin Transporter | Muscarinic acetylcholine receptor | Amitriptyline Hydrochloride | Beta Receptor | psychiatric | Inhibitor | SERT | diseases | Amitriptyline hydrochloride | Sodium Channel | Serotonin Receptor | neuropathic | Histamine Receptor | 5-HTT | mAChR | TrkA/TrkB | SLC6A4 | depression | inhibit | Trk Receptor | Tropomyosin related kinase receptor | Na channels | Na+ channels | pain | Adrenergic Receptor | heterodimerization | 5-HT Receptor | 5-hydroxytryptamine Receptor | neurologic | neurotrophins | Amitriptyline |
| Inhibitors Related | Adiphenine hydrochloride | Phenytoin sodium | Alverine citrate | Dapoxetine hydrochloride | Ribavirin | Famotidine | Lidocaine hydrochloride | L-Aspartic aicd sodium | Alginic acid |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Neuroprotective Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Ion Channel Targeted Library |
United States
