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Tianeptine sodium

5-HT uptake facilitator,selective,antidepressant CAS# 30123-17-2

Tianeptine sodium

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Chemical structure

Tianeptine sodium

3D structure

Chemical Properties of Tianeptine sodium

Cas No. 30123-17-2 SDF Download SDF
PubChem ID 23663953 Appearance Powder
Formula C21H24ClN2NaO4S M.Wt 458.93
Type of Compound N/A Storage Desiccate at -20°C
Solubility H2O : ≥ 235 mg/mL (512.06 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name sodium;7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoate
SMILES CN1C2=CC=CC=C2C(C3=C(S1(=O)=O)C=C(C=C3)Cl)NCCCCCCC(=O)[O-].[Na+]
Standard InChIKey ZLBSUOGMZDXYKE-UHFFFAOYSA-M
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Tianeptine sodium

DescriptionSelective facilitator of 5-HT uptake in vitro and in vivo. Has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant, analgesic and neuroprotective following systemic administration in vivo.

Tianeptine sodium Dilution Calculator

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Tianeptine sodium Molarity Calculator

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Preparing Stock Solutions of Tianeptine sodium

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.179 mL 10.8949 mL 21.7898 mL 43.5796 mL 54.4745 mL
5 mM 0.4358 mL 2.179 mL 4.358 mL 8.7159 mL 10.8949 mL
10 mM 0.2179 mL 1.0895 mL 2.179 mL 4.358 mL 5.4475 mL
50 mM 0.0436 mL 0.2179 mL 0.4358 mL 0.8716 mL 1.0895 mL
100 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.4358 mL 0.5447 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Tianeptine sodium

Selective facilitator of 5-HT uptake in vitro and in vivo. Has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50 > 10 μM) and has no effect on noradrenalin or dopamine uptake. Antidepressant, a

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References on Tianeptine sodium

Formulation of a novel tianeptine sodium orodispersible film.[Pubmed:20532710]

AAPS PharmSciTech. 2010 Sep;11(3):1018-25.

The present investigation was undertaken with the objective of formulating orodispersible film(s) of the antidepressant drug Tianeptine sodium to enhance the convenience and compliance by the elderly and pediatric patients. The novel film former, lycoat NG73 (granular hydroxypropyl starch), along with different film-forming agents (hydroxypropyl methyl cellulose, hydroxyethyl cellulose, and polyvinyl alcohol), in addition to three film modifiers; namely, maltodextrin, polyvinyl pyrrolidone K90 and lycoat RS780 (pregelatinized hydroxypropyl starch) were evaluated. Eight formulae were prepared by the solvent-casting method; and were evaluated for their in vitro dissolution characteristics, in vitro disintegration time, and their physico-mechanical properties. The promising orodispersible film based on lycoat NG73 (F1); showing the greatest drug dissolution, satisfactory in vitro disintegration time and physico-mechanical properties that are suitable for orodispersible films, was evaluated for its bioavailability compared with a reference marketed product (Stablon(R) tablets) in rabbits. Statistical analysis revealed no significant difference between the bioavailability parameters (C(max) (ng/ml), t(max) (h), AUC(0-t) (ng hml(-1)), and AUC(0-infinity) (ng hml(-1))] of the test film (F1) and the reference product. The mean ratio values (test/reference) of C(max) (89.74%), AUC(0-t) (110.9%), and AUC(0-infinity) (109.21%) indicated that the two formulae exhibited comparable plasma level-time profiles. These findings suggest that the fast orodispersible film containing tianeptine is likely to become one of choices for acute treatment of depression.

High-performance liquid chromatographic stability indicating assay method of tianeptine sodium with simultaneous fluorescence and UV detection.[Pubmed:17626716]

J Chromatogr Sci. 2007 Jul;45(6):305-10.

The purpose of this work is to develop a sensitive, selective, and validated stability-indicating HPLC assay of tianeptine (TIA) in bulk drug and tablet form. TIA is subjected to different stress conditions, including UV-light, oxidation, acid base-base hydrolysis, and temperature. TIA and its possible degradation products are analyzed on Agilent-Zorbax-XDB-C18 column using gradient elution with acetonitrile and 0.02M sodium acetate (pH 4.2). The samples are monitored simultaneously with photo-diode array at 254 nm and fluoroscence detector set to 350 nm (ex) and 425 nm (em). TIA is integrated from its UV-chromatogram, and the photodecomposition products are integrated from the fluoroscence-chromatogram. TIA and its photodecomposition products are separated by TLC using ethyl acetate-n-hexane-glacial acetic acid-methanol (10.0:14.0:0.2:1.0, v/v) as developing system. One potential photodegradation product is detected by fluoroscence in TIA-tablet form and separated by TLC. The linear range of TIA is between 0.5 to 50 microg/injection with limits of quantitation and detection values of 30 and 8 ng/injection, respectively. The inter-assay percentage of deviation is not more than 0.03%, and the day-to-day variation is not more than 0.1%.

Pharmacokinetic and bioequivalence assessment of two formulations of tianeptine sodium in healthy male volunteers.[Pubmed:25109511]

Int J Clin Pharmacol Ther. 2014 Sep;52(9):817-23.

BACKGROUND: Tianeptine is widely used for controlling depressive symptoms. OBJECTIVE: The aim of this study was to evaluate the bioequivalence between the generic (test) formulation containing Tianeptine sodium 12.5 mg and the branded (reference) formulation Stablon(R) with regard to their pharmacokinetic profiles. METHODS: A randomized, two-sequence, two-treatment crossover study was conducted in healthy male Korean volunteers. All of the enrolled subjects were allocated to one of two sequence groups. They were administered a tablet of the test or reference formulation and then administered the alternative formulation after a 7-day washout period. The blood samples were taken before dosing and at 0.33, 0.67, 1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, and 10 hours after dosing. The plasma concentrations of tianeptine were analyzed using high-performance liquid chromatography with tandem mass spectrometer. Tolerability was assessed throughout the study. RESULTS: The pharmacokinetic parameters were assessed in the 40 subjects who completed the study. The tianeptine C(max) for the test formulation was 283.13 +/- 57.58 ng/mL (mean +/- SD) and that for the reference formulation was 272.50 +/- 59.00 ng/mL. The AUC(last) of tianeptine was 803.24 +/- 180.94 ngxh/mL for the test formulation and 792.27 +/- 180.93 ngxh/mL for the reference formulation. The geometric mean ratio (%) of the test to reference formulation was 104.04 (90% CI, 99.66 - 108.61) for C(max) and 101.30 (98.01 - 104.71) for AUC(last). Clinically significant adverse events were not reported during the study. CONCLUSION: The test and reference formulations of tianeptine were bioequivalent with regard to the pharmacokinetic parameters of Cmax and AUC(last). Both formulations were tolerated by all of the participants.

Tianeptine sodium salt suppresses TNF-alpha-induced expression of matrix metalloproteinase-9 in human carcinoma cells via suppression of the PI3K/Akt-mediated NF-kappaB pathway.[Pubmed:25168152]

Environ Toxicol Pharmacol. 2014 Sep;38(2):502-9.

Tianeptine sodium salt (TSS) is a selective facilitator of serotonin, but there are no reports regarding anti-invasive effects of TSS. Therefore, we investigated the effect of TSS on the expression of matrix metalloproteinase-9 (MMP-9) and invasion in three different human carcinoma cell lines. Our findings showed that MMP-9 activity was significantly increased in response to tumor necrosis factor-alpha (TNF-alpha), and that TSS reduced TNF-alpha-induced MMP-9 activity in a dose-dependent manner. TSS also downregulated both MMP-9 expression and TNF-alpha-induced MMP-9 promoter activity. Using a matrigel invasion assay, we showed that TSS significantly attenuated invasive rates in TNF-alpha-stimulated LNCaP prostate carcinoma cells. Furthermore, TSS suppressed TNF-alpha-induced NF-kappaB activity, which is a potential transcriptional factor for regulating many invasive genes, including MMP-9, by suppressing IkappaB degradation and nuclear translocation of NF-kappaB subunits in LNCaP prostate carcinoma cells. TSS also downregulated TNF-alpha-induced phosphorylation of phosphatidyl-inositol 3 kinase (PI3K) and Akt, and a selective PI3K/Akt inhibitor, LY294002, diminished TNF-alpha-induced NF-kappaB activation followed by levels of MMP-9, suggesting that TSS also reduces MMP-9 expression by inhibiting the PI3K/Akt-mediated NF-kappaB pathway. These results indicate that TSS is a potential anti-invasive agent by suppression of TNF-alpha-induced MMP-9 expression via inhibition of PI3K/Akt-mediated NF-kappaB activity.

Neuroprotective properties of tianeptine: interactions with cytokines.[Pubmed:12681378]

Neuropharmacology. 2003 May;44(6):801-9.

Tianeptine is an antidepressant with proven clinical efficacy and effects on hippocampal plasticity. Hypoxia increased lactate dehydrogenase (LDH) release from cortical neuronal cultures, and tianeptine (1, 10 and 100 microM) inhibited LDH release as efficiently as the N-methyl-D-aspartate (NMDA) antagonist, MK-801. However, tianeptine did not block apoptosis in cultured cortical neurones caused by NMDA, but reduced apoptosis when interleukin-1beta (IL-1beta) was included with NMDA. In 5-day old mice, intracerebral injection of ibotenate induced reproducible lesions in cortex and white matter. Lesion size was markedly reduced by co-administration of MK-801 (1 mg/kg i.p.) but neither by tianeptine or its enantiomers administered acutely (1, 3 or 10 mg/kg i.p.) nor by tianeptine administered chronically (10 mg/kg i.p. for 5 days). Chronic administration of IL-1beta (10 ng/kg i.p. for 5 days) prior to ibotenate injection exacerbated lesion size in cortex and white matter, and this exacerbation was prevented by chronic pre-treatment with tianeptine (10 mg/kg i.p.) or by acute administration of tianeptine (10 mg/kg i.p.) concomitantly with ibotenate. Thus tianeptine has neuroprotective effects against hypoxia in tissue culture and against the deleterious effects of cytokines in cortex and white matter, but not against NMDA receptor-mediated excitotoxicity.

Analgesic effect of tianeptine in mice.[Pubmed:10227587]

Life Sci. 1999;64(15):1313-9.

The effects of tianeptine, a novel and unusual tricyclic antidepressant drug, on tail-flick and hot-plate tests, which are two thermal analgesia evaluating methods, have been investigated in mice. Tianeptine (5 and 10 mg/kg), para-chlorophenylalanine (pCPA) (100 mg/kg) and a combination of pCPA and tianeptine (10 mg/kg) or saline were injected to mice intraperitoneally. pCPA (100 mg/kg) was injected 24 h before tianeptine or saline treatment when it was combined with tinaeptine (10 mg/kg) or tested alone. The tail-flick latencies and hot-plate reaction times of the mice were measured between 15th and 180th minutes following injections. Tianeptine (10 mg/kg) exhibited a significant antinociceptive activity that could be measured by both tests as compared to groups which were treated with saline or pCPA alone between 15th and 180th min of the observation period. The lower dose of tianeptine (5 mg/kg) or pCPA (100 mg/kg) did not produce any significant changes on tail-flick latency or hot-plate reaction time of the mice. However, pretreatment with pCPA completely blocked the antinociceptive effect induced by tianeptine (10 mg/kg) in both tests used in the present study. Furthermore, tianeptine (10 mg/kg) did not cause any significant impairment effects on rotarod performance of the mice. Our results suggested that tianeptine has a prominent thermal antinociceptive activity in mice and that increased serotonergic activity may be responsible for the analgesic effect of tianeptine.

Neurochemical profile of tianeptine, a new antidepressant drug.[Pubmed:3052825]

Clin Neuropharmacol. 1988;11 Suppl 2:S43-50.

Tianeptine is a new effective antidepressant drug. However, its neurochemical profile in animals differs from that of tricyclic or atypical antidepressants. In the present study, we compared the ex vivo effects of tianeptine on platelet serotonin uptake to those of clomipramine. Ex vivo, after subchronic (15 days, washout 24 h) treatment (10 mg/kg/day i.p.) in rats, tianeptine induced an increase (30%) in [14C]serotonin uptake at a [14C]serotonin concentration of 500 nM while clomipramine induced a decrease (40%) in [14C]serotonin uptake. Stimulation of uptake affected mainly Vmax but not Km. Tianeptine did not inhibit monoamine oxidase (MAO), MAOA or MAOB activity. In vitro, there was no binding of tianeptine to any of the various receptors examined: alpha- and beta-adrenergic, dopamine, serotonin, imipramine, GABA, glutamate, benzodiazepine, muscarinic, histamine, Ca2+ channels. After chronic administration (10 mg/kg/day for 15 days) tianeptine did not alter the concentration (Bmax) or the affinity (Kd) of alpha-2, beta-1, serotonin-1, serotonin-2, imipramine, benzodiazepine, or GABAB receptors. The major effect of tianeptine in rat platelets and synaptosomes is a small increase in 5-HT uptake after subchronic administration.

Description

Tianeptine sodium salt is a selective facilitator of 5-HT uptake in vitro and in vivo.

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