Tianeptine Metabolite MC5 sodium

Description: Tianeptine metabolite MC5, an active derivative of the atypical antidepressant tianeptine produced through beta-oxidation, exhibits selective G protein activation in bioluminescence resonance energy transfer (BRET) assays. Utilizing HEK293T cells expressing the human µ-opioid receptor (MOR) over the human delta-opioid receptor (DOR, EC50s = 0.454 and >100 µM, respectively), it demonstrates specificity. Moreover, this metabolite reduces immobility in wild-type mice during the forced swim test at a dose of 30 mg/kg, an effect not observed in MOR knockout mice, suggesting its antidepressant-like activity is MOR-dependent. Smiles: O=C(CCCCNC1C2=C(N(S(=O)(C3=CC(Cl)=CC=C31)=O)C)C=CC=C2)[O-].[Na+]