Amitriptyline-d 6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride ( HY-B0527A ). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride 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 hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis ). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K i = 2.58 μM). Amitriptyline hydrochloride 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 hydrochloride can block sodium channels and hERG potassium channel ( IC 50 = 4.78 μM) and it has cardiotoxicity.
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