Amitriptyline

Description

Amitriptyline is an orally active tricyclic antidepressant TCA . Amitriptyline mainly exerts its antidepressant effect by blocking SERT Ki = 3.45 nM and NET Ki = 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 ?2A 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 Ki = 2.58 ?M . Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors M1/M2/M3/M4/M5 receptors Ki = 11-24 nM , H1 receptors Ki = 0.5-1.1 nM , adrenergic ?1 receptors Ki = 4.4 nM , etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel IC50 = 4.78 ?M and it has cardiotoxicity.