Tianeptine sodium

Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.

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Tianeptine sodium Chemical Structure

Tianeptine sodium Chemical Structure
Molecular Weight: 458.93

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Product Description

Biological Activity

Description Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.
Targets 5-HT [1]
In vitro
In vivo Tianeptine treatment prevents the CMS-induced increase in corticotropin-releasing factor (CRF) mRNA levels in the dBNST, and reduces corticotropin-releasing factor (CRF) mRNA levels in dBNST in non-stressed rats. Tianeptine treatment significantly decreases CRF mRNA levels in the ventral BNST and CeA of non-stressed controls as well as CMS-exposed rats. [1] Tianeptine blocks the stress-induced suppression of PB potentiation in CA1 without affecting the stress-induced enhancement of LTP in basolateral nucleus (BLA) of the amygdala in anesthetized rats. Tianeptine administered under non-stress conditions enhances PB potentiation in the hippocampus and LTP in the amygdala in anesthetized rats. [2] Tianeptine attenuates the behavioral signs of sickness behavior induced by peripheral, but not central, LPS or IL-1beta in the rats. [3] Tianeptine results in a normalized scaling of the amplitude ratio of NMDA receptor to AMPA/kainate receptor-mediated currents and prevents the stress-induced attenuation of NMDA-EPSCs deactivation in rats. [4] Tianeptine treatment significantly reduces apoptosis in the temporal cortex and dentate gyrus, both in control and stressed animals, but has no effect in the Ammons Horn. [5] Tianeptine (2.5 mg/kg, i.v.) increases the extracellular dopamine only in the nucleus accumbens. Tianeptine significantly raises the extracellular concentrations of dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in both nucleus accumbens and striatum. [6]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kim SJ, et al. Neuropharmacology, 2006, 50(7), 824-833.

[2] Vouimba RM, et al. Stress, 2006, 9(1), 29-40.

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Chemical Information

Download Tianeptine sodium SDF
Molecular Weight (MW) 458.93
Formula

C21H24ClN2NaO4S

CAS No. 30123-17-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 91 mg/mL (198.28 mM)
Water 91 mg/mL (198.28 mM)
Ethanol 91 mg/mL (198.28 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Heptanoic acid, 7-[(3-chloro-6,11-dihydro-6-methyl-5,5-dioxidodibenzo[c,f][1,2]thiazepin-11-yl)amino]-, sodium salt (1:1)

Research Area

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Rating
Source Br J Haematol 2014 4, e411. Tianeptine sodium purchased from Selleck
Method Bioluminescence resonance energy transfer
Cell Lines Mouse MOR
Concentrations 23.3?.9 nM
Incubation Time
Results In addition, the tianeptine-induced activation of MOR was blocked by the opioid antagonist naltrexone in a dose-dependent manner.

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