Amitriptyline

Overview

Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT ( K i = 3.45 nM) and NET ( K i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine ( 5-HT ) and norepinephrine ( NE ) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis ). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) ( K i = 11-24 nM), H1 receptors ( K i = 0.5-1.1 nM), adrenergic α1 receptors ( K i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel ( IC 50 = 4.78 μM) and it has cardiotoxicity.

Application

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Product Information

• Catalog No.: HY-B0527
• CAS No.: 50-48-6
• Molecular Formula: C20H23N
• Molecular Weight: 277.40
• Purity: 99.93%
• Storage: 4°C, protect from light * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
• Solubility: ≥ 2.5 mg/mL (9.01 mM); Clear solution
• Availability: In-stock

Source

Original product source