Formulation: A solid
Formal Name: 7-[(3-chloro-6,11-dihydro-6-methyl-5,5-dioxidodibenzo[c,f][1,2]thiazepin-11-yl)amino]-heptanoic-4,4,5,5,6,6-d6 acid, monohydrochloride
Purity: ≥99% deuterated forms (d1-d6)
Formula Markup: C21H19ClD6N2O4S • HCl
Formula Weight: 479,5
Shelf life (days): 1460
Notes: Tianeptine-d6 is intended for use as an internal standard for the quantification of tianeptine (Item No. 17561) by GC- or LC-MS. Tianeptine is an atypical antidepressant.{28646} 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.{28646,28645} 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.{43567} 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.{43568} 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.{43569} It also reverses increases in extracellular glutamate levels induced by acute restraint stress in the basolateral nucleus of the amygdala in rats.{43570}
English
Deutsch
