Tianeptine powder (66981-73-5)

01 Overview

Tianeptine, a tricyclic compound, is a selective facilitator of 5-HT (serotonin; sc-201146) uptake in vitro and in vivo. Additionally, Tianeptine is reported to act as a selective inhibitor of dopamine uptake and is similar to amineptine. Tianeptine does not have a noted effect on monoamine uptake. In a study utilizing purified synaptosomes from rat brain, Tianeptine was reported to enhance serotonin uptake in selective brain regions. Purified synaptosomes were obtained from rats and incubated with tritium-labeled 5-H and Tianeptine in vitro . The synaptosomes were then analyzed for uptake and release of 5-HT via a liquid scintillation counter.

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03 Tianeptine powder (66981-73-5) video

04 Tianeptine powder (66981-73-5) Base Information

Name: Tianeptine powder

CAS: 66981-73-5

Purity: 98%

Chemical name: 7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid

Synonyms: S-1574; JNJ-39823277; TPI-1062

Molecular Formula: C21H25ClN2O4S

Molecular Weight: 436.95

Melting Point: 129-131°C

InChI Key: JICJBGPOMZQUBB-UHFFFAOYSA-N

Form: Powder

Appearance: White Color

Half Life: 4 to 9 hours

Solubility: Freely soluble in water, in methanol and in methylene chloride.

Storage Condition: Store at 4° C

Application: Tricyclic compound with psychostimulant, anti-ulcer and anti-emetic properties. Antidepressant

Testing Document: Available 

05 Tianeptine powder (66981-73-5) General Description

Tianeptine is a drug used primarily in the treatment of major depressive disorder and has been studied in the treatment of irritable bowel syndrome (IBS).Structurally, Tianeptine, is an atypical antidepressant which is used mainly in the treatment of major depressive disorder, although it may also be used to treat anxiety, asthma, and irritable bowel syndrome.

Tianeptine has antidepressant and anxiolytic effect with a relative lack of sedative, anticholinergic, and cardiovascular side effects. It has been found to act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors as do most tricyclic antidepressants (TCA).

06 Tianeptine powder (66981-73-5) History

Tianeptine was discovered and patented by the French Society of Medical Research in the 1960s. Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in a number of other European countries under the trade name Coaxil as well as in Asia (including Singapore) and Latin America as Stablon and Tatinol but it is not available in Australia, Canada, New Zealand, the United Kingdom, or the United States.

07 Tianeptine powder (66981-73-5) Mechanism Of Action

Recent studies suggest that tianeptine acts as a full agonist at the mu-type opioid receptor (MOR) [A33314], [A33316]. The mu opioid receptors are currently being studied as effective targets for antidepressant therapies. It is believed that the clinical effects of tianeptine are owed to its modulation of these receptors.

Many demonstrate that the mechanism of action of tianeptine is distinct from SSRIs and support the hypothesis that the mechanism of action of tianeptine relates to alteration of glutaminergic activity in the amygdala and the hippocampus [A31971, A431969, A31986]. In addition to the above mechanisms, tianeptine is a unique antidepressant and anxiolytic medication that stimulates the uptake of serotonin (5-hydroxytryptamine; 5-HT), and 5-hydroxyindoleacetic acid (5-HIAA) in brain tissue [A31971]. Although the monoaminergic neurotransmitters serotonin (5-HT), noradrenaline (NA) and dopamine (DA) are proven to be related to the occurrence of depressive disorders, it is now recognized that monoamine deficits are not sufficient to explain the mechanism of action of antidepressant.

08 Tianeptine powder (66981-73-5) Application

· 1) Tianeptine Improves Depressive Symptoms

· 2) Tianeptine Lessens Anxiety, Stress, and PTSD and Symptoms From Stress.

· 3) Tianeptine Benefits Memory and Learning

· 4) Tianeptine is an Anti-inflammatory

· 5) Tianeptine decreases pain

· 6) Tianeptine Helps Treat Irritable bowel Syndrome

· 7) Tianeptine Reduces Asthma

09 Tianeptine powder (66981-73-5) More research

A clinical trial comparing its efficacy and tolerability with amitriptyline in the treatment of irritable bowel syndrome showed that tianeptine was at least as effective as amitriptyline and produced less prominent adverse effects such as dry mouth and constipation.Tianeptine has been reported to be very effective for asthma. In August 1998, Dr. Fuad Lechin and colleagues at the Central University of Venezuela Institute of Experimental Medicine in Caracas published the results of a 52-week randomized controlled trial of asthmatic children; the children in the groups that received tianeptine had a sharp decrease in clinical rating and increased lung function. Two years earlier, they had found a close, positive association between free serotonin in plasma and severity of asthma in symptomatic persons. As tianeptine was the only agent known to both reduce free serotonin in plasma and enhance uptake in platelets, they decided to use it to see if reducing free serotonin levels in plasma would help. By November 2004, there had been two double-blind placebo-controlled crossover trials and a >25,000 person open-label study lasting over seven years, all showing effectiveness. Tianeptine also has anticonvulsant and analgesic effects, and a clinical trial in Spain that ended in January 2007 has shown that tianeptine is effective in treating pain due to fibromyalgia. Tianeptine has been shown to have efficacy with minimal side effects in the treatment of attention-deficit hyperactivity disorder.

10 Tianeptine powder (66981-73-5) Document Download

COA

11 Tianeptine powder (66981-73-5) Reference

· Mennini, T., et al. 1987. Naunyn Schmiedebergs Arch. Pharmacol. 336: 478-482. PMID: 3437921

· Kato, G. and Weitsch, A.F. 1988. Clin Neuropharmacol. 11: S43-S50. PMID: 3052825

· Tianeptine Sodium. Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. 5 December 2011. Retrieved 2 December 2013.

· J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 1195–. ISBN 978-1-4757-2085-3.

12 PRECAUTION AND DISCLAIMER:

PRECAUTION AND DISCLAIMER:

This Material is Sold For Research Use Only. Terms of Sale Apply. Not for Human Consumption, nor Medical, Veterinary, or Household Uses.