Amitriptyline hydrochlorideAmitriptyline hydrochloride
MedChemExpress (MCE)
HY-B0527A
549-18-8
98.91%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
Amitriptyline hydrochloride (30 min) protects hippocampal neurons (T17 cells) from apoptosis (EC50: 50 nM)[3]. Amitriptyline hydrochloride (0.5 μM, 30 min) induces TrkA and TrkB receptor phosphorylation and activation in hippocampal neurons[3]. Amitriptyline hydrochloride (500 nM, 5 days) induces neurite outgrowth in PC12 cells[3].
Amitriptyline (15 mg/kg, i.p.) hydrochloride activates TrkA and TrkB receptors, and prevents Kainic acid (HY-N2309)-induced neuronal apoptosis in brain of C57BL/6 mice[3]. Amitriptyline (15-25 mg/kg, i.p., 5 days) hydrochloride induces TrkA and TrkB hetero-dimerization in mouse brain[3]. Amitriptyline (15 mg/kg, i.p.) hydrochloride shows antinociceptive effect by activation of α2-adrenoceptors in mice[3].
5-HT1A Receptor 450 nM (IC50) 5-HT1B Receptor 40 nM (IC50) 5-HT2A Receptor 4 nM (IC50) 5-HT2B Receptor 40 nM (IC50) 5-HT2C Receptor 6 nM (IC50) H1 Receptor 1.1 nM (IC50) H3 receptor 1 μM (IC50) H4 receptor 33.6 nM (IC50) SERT 3.45 nM (Ki) NET 13.3 nM (Ki) DAT 2.58 μM (Ki) Adrenergic receptor 24 nM (IC50) muscarinic receptor 7.2 nM (IC50) TrkA TrkB
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[1]. Kim Lawson. A Brief Review of the Pharmacology of Amitriptyline and Clinical Outcomes in Treating Fibromyalgia. Biomedicines. 2017 Jun
5(2): 24. [Content Brief]
[2]. S Neil Vaishnavi , et al. Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. Biol Psychiatry. 2004 Feb 1
55(3):320-2. [Content Brief]
[3]. Jang, S.W., et al., Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity. Chem Biol, 2009. 16(6): p. 644-56. [Content Brief]
[4]. Ghelardini C, et al. Antinociception induced by amitriptyline and imipramine is mediated by alpha2A-adrenoceptors. Jpn J Pharmacol. 2000 Feb
82(2):130-7. [Content Brief]