Tianeptine (sodium salt)

Tianeptine is an atypical antidepressant.¹ It is an agonist of the μ-opioid receptor (MOR; EC₅₀s = 194 and 641 nM for human and mouse receptors, respectively, in a BRET assay for G protein activation) and also has effects on the glutamate system.^1,2 Tianeptine (30 mg/kg) decreases immobility in the forced swim test in wild-type, but not MOR knockout mice, indicating antidepressant-like activity dependent on MORs.³ It increases locomotor activity at a dose of 30, but not 10 mg/kg, in the open field test and increases paw withdrawal latency in the hot-plate test in mice. Tianeptine modulates AMPA receptor activity by increasing phosphorylation of the AMPA receptor GluR1 subunit in the frontal cortex and hippocampal CA3 region in mice.⁴ It prevents increases in glial glutamate transporter 1 (GLT-1) expression induced by chronic restraint stress in the hippocampal CA3 region in rats when administered at a dose of 10 mg/kg per day for 21 days.⁵ It also reverses increases in extracellular glutamate levels induced by acute restraint stress in the basolateral nucleus of the amygdala in rats.⁶

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1. McEwen, B.S., Chattarji, S., Diamond, D.M., et al. The neurobiological properties of tianeptine (Stablon): From monoamine hypothesis to glutamatergic modulation. Mol. Psychiatry 15(3), 237-249 (2010).

2. Gassaway, M.M., Rives, M.L., Kruegel, A.C., et al. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. Transl. Psychiatry 4(7), e411 (2014).

3. Samuels, B.A., Nautiyal, K.M., Kruegel, A.C., et al. The behavioral effects of the antidepressant tianeptine require the mu-opioid receptor. Neuropsychopharmacology 42(10), 2052-2063 (2017).

4. Svenningsson, P., Bateup, H., Qi, H., et al. Involvement of AMPA receptor phosphorylation in antidepressant actions with special reference to tianeptine. Eur. J. Neurosci. 26(12), 3509-3517 (2007).

5. Reagan, L.P., Rossell, D.R., Wood, G.E., et al. Chronic restraint stress up-regulates GLT-1 mRNA and protein expression in the rat hippocampus: Reversal by tianeptine. Proc. Natl. Acad. Sci. USA 101(7), 2179-2184 (2004).

6. Reznikov, L.R., Grillo, C.A., Piroli, G.G., et al. Acute stress-mediated increases in extracellular glutamate levels in the rat amygdala: Differential effects of antidepressant treatment. Eur. J. Neurosci. 25(10), 3109-3114 (2007).

Szafarz, M., Wencel, A., Pociecha, K., et al. Pharmacokinetic study of tianeptine and its active metabolite MC5 in rats following different routes of administration using a novel liquid chromatography tandem mass spectrometry analytical method. Naunyn Schmiedebergs Arch. Pharmacol. 391(2), 185-196 (2017).