受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H23N.HCl |
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分子量 | 313.86 | CAS No. | 549-18-8 | ||||
Solubility (25°C)* | 体外 | DMSO | 63 mg/mL (200.72 mM) | ||||
Ethanol | 63 mg/mL (200.72 mM) | ||||||
Water | 15 mg/mL (47.79 mM) | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
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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] |
Evidence for Specific Receptor-Mediated Toxicity of Pharmaceuticals in Aquatic Organisms Derived from Acute and Chronic Standard Endpoints [ Environ Toxicol Chem, 2021, 10.1002/etc.5018] | PubMed: 33595135 |
Identification of amitriptyline HCl, flavin adenine dinucleotide, azacitidine and calcitriol as repurposing drugs for influenza A H5N1 virus-induced lung injury. [ PLoS Pathog, 2020, 16;16(3):e1008341] | PubMed: 32176725 |
Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. [ Sci Rep, 2018, 8(1):15753] | PubMed: 30361678 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。