Escitalopram

Escitalopram is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and the (S) isomer of citalopram (Item No. 14572) and (R)-citalopram.¹ It selectively binds to SERT (K_i = 0.89 nM) over the norepinephrine and dopamine transporters (K_is = >10,000 and 8,150 nM, respectively) and inhibits 5-HT reuptake in rat brain synaptosomes (IC₅₀ = 2.1 nM).^2,3 Escitalopram reduces immobility in the forced swim test in mice (ED₅₀ = 12 mg/kg), indicating anti-depressant-like activity, and increases exploratory behavior in the black-and-white box test in mice with a minimal effective dose (MED) of 0.49 mg/kg, indicating anxiolytic-like activity.⁴ Escitalopram (20 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 (Item No. 10681).⁵ Formulations containing escitalopram have been used in the treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD).

WARNING This product is not for human or veterinary use.

1. Höschl, C., and Svestka, J. Escitalopram for the treatment of major depression and anxiety disorders. Expert Rev. Neurother. 8(4), 537-552 (2008).

2. Zhang, P., Cyriac, G., Kopajtic, T., et al. Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters. J. Med. Chem. 53(16), 6112-6121 (2010).

3. Sánchez, C., Bøgesø, K.P., Ebert, B., et al. Escitalopram versus citalopram: The surprising role of the R-enantiomer. Psychopharmacology (Berl) 174(2), 163-176 (2004).

4. Sánchez, C., Bergqvist, P.B.F., Brennum, L.T., et al. Escitalopram, the S-(+)-enantiomer of citalopram, is a selective serotonin reuptake inhibitor with potent effects in animal models predictive of antidepressant and anxiolytic activities. Psychopharmacol. (Berl) 167(4), 353-362 (2003).

5. Carpinteiro, A., Edwards, M.J., Hoffmann, M., et al. Pharmacological inhibition of acid sphingomyelinase prevents uptake of SARS-CoV-2 by epithelial cells. Cell Rep. Med. 1(8), 100142 (2020).