Tianeptine

Catalog No.S5087 Synonyms: S-1574, JNJ-39823277, TPI-1062

Tianeptine Chemical Structure

Molecular Weight(MW): 436.95

Tianeptine is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors.

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Biological Activity

Description Tianeptine is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors.
Targets
5-HT [2]
()
μ-opioid receptor [1]
(for human μ-opioid receptor)
383 nM(Ki)
In vitro

Tianeptine modulates glutamatergic transmission. It restores stress-induced reduction of dendritic arborization in hippocampal neurons and reverses stress-induced inhibition of long-term potentiation at excitatory synapses in the hippocampus and prefrontal cortex[1]. Tianeptine is a serotonin reuptake enhancer and has an antidepressant efficacy[2].

In vivo In preclinical studies, tianeptine has beneficial effects in a number of behavioral models related to depression, anxiety and other stress-related disorders[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Adult male Sprague-Dawley rats
  • Formulation: 0.9% saline
  • Dosages: 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (199.1 mM)

* 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 Information

Molecular Weight 436.95
Formula

C21H25ClN2O4S

CAS No. 72797-41-2
Storage powder
in solvent
Synonyms S-1574, JNJ-39823277, TPI-1062

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01309776 Completed Major Depressive Disorder Samsung Medical Center March 2011 Phase 4
NCT02103985 Completed Healthy Johnson & Johnson Pharmaceutical Research & Development L.L.C. May 2009 Phase 1
NCT02049697 Completed Healthy Johnson & Johnson Pharmaceutical Research & Development L.L.C. April 2009 Phase 1
NCT00879372 Unknown status Bipolar Disorder Hospital de Clinicas de Porto Alegre|Conselho Nacional de Desenvolvimento Científico e Tecnológico|Stanley Medical Research Institute March 2009 Phase 3

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Opioid Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID