Sertraline hydrochloride

Sertraline is a tetraline that inhibits monoamine transporters and acts as a potent highly selective serotonin reuptake inhibitor (SSRI), with affinity for the serotonin transporter (SERT), increasing availability of serotonin (5-hydroxytryptamine, 5-HT) in the brain and leading to antidepressant, anxiolytic and antiobsessional effects. Sertraline binds also to the dopamine transporter (DAT) and the sigma1 receptor (but not the sigma2 receptor) with 100-fold lower affinity. It acts as an antagonist of the sigma1 receptor, and is able to reverse sigma1 receptor-dependent actions of fluvoxamine, a potent agonist of the receptor, in vitro. Sertraline displays antiproliferative activity on human colorectal carcinoma cells.