Tianeptine-d₁₂ 

Tianeptine-d₁₂ is a deuterated analog of Tianeptine (HY-90003).Tianeptine is an atypical antidepressant. Tianeptine is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

449.03

C₂₁H₁₃D₁₂ClN₂O₄S

1189870-26-5

72797-41-2

N(C(C(C(C(C(C(C(O)=O)([2H])[2H])([2H])[2H])([2H])[2H])([2H])[2H])([2H])[2H])([2H])[2H])C1C=2C(S(=O)(=O)N(C)C=3C1=CC=CC3)=CC(Cl)=CC2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Wagstaff A J, et al. Tianeptine: a review of its use in depressive disorders[J]. CNS drugs, 2001, 15: 231-259.

  [3]. Plaisant F, et al. Neuroprotective properties of tianeptine: interactions with cytokines[J]. Neuropharmacology, 2003, 44(6): 801-809.  [Content Brief]

  [4]. Sharma A K, et al. Effects of calcium channel blocker, nifedipine, on antidepressant activity of fluvoxamine, venlafaxine and tianeptine in mice[J]. Int J Basic Clin Pharmacol, 2015, 4: 1-7.