Sertraline-d3 (hydrochloride)

Sertraline-d₃ is intended for use as an internal standard for the quantification of sertraline by GC- or LC-MS. Sertraline is a selective serotonin reuptake inhibitor (SSRI).^1,2 It inhibits monoamine uptake by the serotonin transporter (SERT) with an IC₅₀ value of 70 nM.¹ It is selective for SERT over the norepinephrine and dopamine transporters (IC₅₀s = 520 and 720 nM, respectively). Sertraline (3.2-56 mg/kg, s.c.) reduces immobility in the forced swim test in mice.² Sertraline (5 µM) prevents acid sphingomyelinase activation and subsequent ceramide release induced by infection with replication-deficient vesicular stomatitis virus pseudoviral particles (pp-VSV) presenting the severe acute respiratory coronavirus 2 (SARS-CoV-2) spike protein in Vero cells, an effect that can be overcome with exogenous application of C16 ceramide.³ Formulations containing sertraline have been used in the treatment of depression, obsessive-compulsive disorder (OCD), premenstrual dysphoric disorder (PMDD), and various anxiety disorders.

1.Welch, W.M., Kraska, A.R., Sarges, R., et al.Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralinsJ. Med. Chem.27(11)1508-1515(1984) 2.Koe, B.K., Weissman, A., Welch, W.M., et al.Sertraline, 1S,4S-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, a new uptake inhibitor with selectivity for serotoninJ. Pharmacol. Exp. Ther.226(3)686-700(1983) 3.Carpinteiro, A., Edwards, M.J., Hoffmann, M., et al.Pharmacological inhibition of acid sphingomyelinase prevents uptake of SARS-CoV-2 by epithelial cellsCell Rep. Med.1(8)100142(2020)