Sertraline HCl

Description: Sertraline HCl (formerly CP 51, 974-1; CP 51974-1; CP-51, 974; trade names: Sealdin; Adjuvin; Atruline; Gladem; Tatig; Tresleen; Zoloft), the hydrochloride salt of Sertraline, is a potent and marketed antidepressant drug acting as a 5-HT serotonin receptor antagonist with Ki of 13 nM. Sertraline is primarily a serotonin reuptake inhibitor (SRI) with a binding affinity towards the serotonin transporter of Ki=2.8 nM. Sertraline exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, Sertraline is less selective for blocking 5-HT uptake, relative to DA uptake than these agents. Sertraline is also a dopamine reuptake inhibitor, (< 50 nmol/L). However, this is not considered a tight binding, and this action is only 10% of its potency as a monoamine reuptake inhibitor. It is a sigma1 receptor agonist with 5% of its SRI potency, and an alpha1-adrenoreceptor antagonist with 1–10% of its SRI potency.

References: J Pharmacol Exp Ther. 1983 Sep; 226(3):686-700.

Related CAS: 79617-96-2 (free base) 79559-97-0 (HCl)