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Amitriptyline hydrochloride

SKU: orb1310394

Description

Amitriptyline hydrochloride

Research Area

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

Images & Validation

Key Properties

CAS Number549-18-8
MW313.86
Purity97.00%
FormulaC20H24ClN
SMILESCl.CN(C)CC\C=C1\c2ccccc2CCc2ccccc12
TargetNorepinephrine,Serotonin Transporter,Sigma receptor,Adrenergic Receptor,Histamine Receptor,Sodium Channel,5-HT Receptor,AChR,Trk receptor
SolubilityEthanol: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 decrease 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 increase the total distance travelled of mice in novel cages. Amitriptyline (10 mg/kg p.o., twice daily) considerably attenuate 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]
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 bind 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

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
DisclaimerFor 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

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Key Properties

No computed properties available.

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Amitriptyline hydrochloride (orb1310394)

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5 g
$ 70.00
1 ml x 10 mM (in DMSO)
$ 80.00
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