Tianeptine (sodium salt)

Tianeptine is an atypical antidepressant. 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. 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. 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. 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. It also reverses increases in extracellular glutamate levels induced by acute restraint stress in the basolateral nucleus of the amygdala in rats.Formal Name: 7-[(3-chloro-6,11-dihydro-6-methyl-5,5-dioxidodibenzo[c,f][1,2]thiazepin-11-yl)amino]-heptanoic acid, monosodium salt. CAS Number: 30123-17-2. Molecular Formula: C21H24ClN2O4S . Na. Formula Weight: 458.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: [O-]C(CCCCCCNC(C1=C2C=C(Cl)C=C1)C(C=CC=C3)=C3N(C)S2(=O)=O)=O.[Na+]. InChi Code: InChI=1S/C21H25ClN2O4S.Na/c1-24-18-9-6-5-8-16(18)21(23-13-7-3-2-4-10-20(25)26)17-12-11-15(22)14-19(17)29(24,27)28,/h5-6,8-9,11-12,14,21,23H,2-4,7,10,13H2,1H3,(H,25,26),/q,+1/p-1. InChi Key: ZLBSUOGMZDXYKE-UHFFFAOYSA-M.