Amitriptyline HCl

製品コードS3183 バッチS318301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H23N.HCl
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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.000mg/ml (12.74mM) Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Amitriptyline HCl は、セロトニントランスポーター (SERT) およびノルエピネフリントランスポーター (NET) の両方の阻害剤であり、Ki 値はそれぞれ 3.45 nM および 13.3 nM です。Amitriptyline HCl はまた、ヒスタミン受容体 H1、ヒスタミン受容体 H4、5-HT2 および sigma 1 receptor も阻害し、Ki 値はそれぞれ 0.5 nM、7.31 nM、235 nM および 287 nM です。アミトリプチリンは三環系抗うつ薬 (TCA) です。
in vitro

Amitriptyline inhibits Forskolin-stimulated cyclic AMP accumulation with EC50 values of 16.2 μM in intact CHO/DOR cells. This compound causes a concentration-dependent stimulation of ERK1/2 and GSK-3β phosphorylation with EC50 values of 9.0 μM in CHO/DOR cells. It (15 μM) causes a stimulation of ERK1/2 phosphorylation in C6 cells. This chemical (30 μM) inhibits Forskolin-stimulated adenylyl cyclase activity and antagonizes (−)-U50,488 inhibitory effect in rat nucleus accumbens. It binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization. This compound (< 500 nM) promotes TrkA autophosphorylation in primary neurons and induces neurite outgrowth in PC12 cells. It selectively protects T17 cells from apoptosis with EC50 of 50 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. This compound (15 mg/kg and 30 mg/kg, i.p.) dose-dependently decreases the immobility time in the forced swimming test (FST) of mice. This chemical (15 mg/kg, i.p.) shows a significant 24-h rhythm in the immobility time in the forced swimming test (FST) of mice. It (1 mg/kg and 3 mg/kg) significantly increases the total distance travelled of mice in novel cages. This compound (10 mg/kg p.o., twice daily) considerably attenuates the hypothermic response to 8-OHDPAT and mCPP in mice. It (10 mg/kg p.o., twice daily) significantly reduces serotonin transporter density by approximately 20% in cortex of mice.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/14744476/
  • https://pubmed.ncbi.nlm.nih.gov/11179435/
  • https://pubmed.ncbi.nlm.nih.gov/11561066/
  • https://pubmed.ncbi.nlm.nih.gov/17689532/
  • https://pubmed.ncbi.nlm.nih.gov/19828880/
  • https://pubmed.ncbi.nlm.nih.gov/19549602/
  • https://pubmed.ncbi.nlm.nih.gov/16079297/
  • https://pubmed.ncbi.nlm.nih.gov/16032412/
  • https://pubmed.ncbi.nlm.nih.gov/16782354

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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