Amitriptyline [CAS 50-48-6]

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 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 Ki = 2.58 μM) . 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 α1 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 μM) and it has cardiotoxicity[1][2][3][4][5].

[50-48-6]

C20H23N

277.4

CN(CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3)C

5-HT Receptor; Adrenergic Receptor; Apoptosis; Dopamine Transporter; Histamine Receptor; mAChR; Potassium Channel; Serotonin Transporter; Sodium Channel; Trk Receptor

5-HT Receptor; Histamine Receptor; TrkA; TrkB

10mM

99.94

DMSO : 100 mg/mL (ultrasonic)

4°C (Powder, protect from light)

Room Temperature

H302-H315-H319-H335

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501