Tianeptine Sulfate

**Product Name:** Tianeptine Sulfate

**Synonyms:** Tianeptine hemisulfate monohydrate; THM; 7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid hemisulfate monohydrate

**General Description:** Tianeptine sulfate is formally described as 7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid (sulfate salt). It is an atypical tricyclic compound. While tianeptine is utilized clinically in several European, Latin American, and Asian countries as an antidepressant and anxiolytic (typically administered as the highly hygroscopic sodium salt under the trade names Stablon or Coaxil), the sulfate salt formulation is notable for its improved chemical stability and a prolonged pharmacokinetic half-life. In analytical, clinical, and forensic toxicology, tianeptine sulfate is utilized as a reference standard for the calibration of analytical instrumentation (such as LC-MS/MS and GC-MS) and the development of screening methodologies to identify and quantify the substance in seized materials, illicit dietary supplements, or biological matrices.

**Technical Information (Hemisulfate Monohydrate):** *

**CAS Number:** 1224690-84-9 (Hemisulfate monohydrate) / 66981-73-5 (Free acid) * **Molecular Formula:** C₄₂H₅₆Cl₂N₄O₁₄S₃ *[2(C₂₁H₂₅ClN₂O₄S) • H₂SO₄ • 2(H₂O)]* *

**Formula Weight:** 1008.0 g/mol * **SMILES:** CN1C2=CC=CC=C2C(C3=C(S1(=O)=O)C=C(C=C3)Cl)NCCCCCCC(=O)O (Free acid) * **InChI Key:** KVVMXNNJBVTOSX-UHFFFAOYSA-N *

**Formulation:** Typically supplied as a neat white crystalline solid or as a certified reference material solution (e.g., 1 mg/mL in methanol). **Biological Action:*

* Historically mischaracterized as a selective serotonin reuptake enhancer (SSRE), more recent pharmacological profiling has revealed that tianeptine is an atypical, full agonist at the μ-opioid receptor (MOR), with weaker activity at the δ-opioid receptor (DOR). It also modulates the glutamatergic system, affecting AMPA and NMDA receptor transmission, which is believed to mediate its neuroplastic and antidepressant effects at therapeutic doses. At supratherapeutic doses, its opioid receptor agonism drives significant abuse potential, yielding euphoria, respiratory depression, and classic opioid-like withdrawal syndromes.

**Regulatory and Safety Information:** *

**Intended Use:** This product is intended strictly for use as an analytical reference standard for forensic, toxicological, and academic research purposes.
* **Warning:** **This product is not for human or veterinary use.** *

**Legal Status:** The regulatory status of tianeptine varies widely. In the United States, tianeptine is not approved by the Food and Drug Administration (FDA) for any medical use. Due to severe cases of toxicity, withdrawal, and a surge in illicit use (where it is often colloquially marketed in gas stations and online as a “legal high” or “gas station heroin”), tianeptine and its salts have been placed under strict control as Schedule I or Schedule II substances in numerous U.S. states (including Alabama, Florida, Michigan, Tennessee, and others). It is also heavily regulated or banned in various European countries. Procurement may require relevant local licenses. Handling should only occur within professional laboratory environments using appropriate Personal Protective Equipment (PPE) such as safety glasses, chemical-resistant gloves, and a laboratory coat.