{"id":3913,"date":"2025-09-07T00:23:52","date_gmt":"2025-09-07T00:23:52","guid":{"rendered":"https:\/\/modafinil.pl\/?post_type=product&p=3913"},"modified":"2026-10-06T11:02:09","modified_gmt":"2026-10-06T11:02:09","slug":"tianeptine-acid-form-tianeptine-acid","status":"publish","type":"product","link":"https:\/\/modafinil.pl\/en\/sklep\/tianeptine-acid-form-tianeptine-acid\/","title":{"rendered":"Tianeptine, Acid Form \/ Tianeptine Acid (CAS 66981-73-5) \u2014 Chemical Reagent 1000 mg, Purity \u2265 99.41%"},"content":{"rendered":"

7-{[3-Chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl]amino}heptanoic acid<\/strong>, crystalline powder, 1000 mg package. Material intended exclusively for in vitro laboratory and analytical research<\/strong>. The product is not intended for consumption by humans or animals<\/strong>, is not a medicinal product, a dietary supplement, a foodstuff, or a cosmetic.<\/p>\n

Three Different Entities That Must Not Be Confused<\/h2>\n

For this molecule, separating the layers is especially important, because the acid form offered here is not the same catalog entity as the active substance of the registered drug — even the PubChem database lists them under separate identifiers. Three contexts, three entirely different statuses:<\/p>\n\n\n\n\n\n\n\n
Separating the layers: substance — medicinal product — reagent<\/caption>\n
Entity<\/th>\nWhat it is<\/th>\nWhat it concerns<\/th>\n<\/tr>\n<\/thead>\n
Chemical substance, acid form
tianeptine, CAS 66981-73-5<\/th>\n		A chemical concept — the free acid, the parent form of the salts used pharmaceutically. On its own it is neither a drug nor a reagent; status is conferred only by the form in which it was manufactured and approved. PubChem catalogs this entry (CID 68870) with a clinical development status marked as phase 0 — preclinical.<\/td>\nchemistry, substance registries<\/td>\n<\/tr>\n
Medicinal product
tianeptine salt (including sodium), marketed among others as Coaxil, Stablon<\/th>\n		A pharmaceutical preparation: a defined pharmaceutical form, manufacturing under GMP conditions, a registration dossier, safety monitoring, catalogued under a different PubChem\/CAS identifier than the free acid. It does not hold marketing authorization as a medicinal product in Poland.<\/strong><\/td>\nthis is the entity to which the clinical trials in humans referred<\/strong><\/td>\n<\/tr>\n
Chemical reagent
the material offered here<\/th>\n		Material for laboratory and analytical work, in free-acid form. It does not hold, and cannot hold, approval for use in humans or animals<\/strong> — it has no pharmaceutical form and no medicinal product documentation.<\/td>\nanalytics, chemistry, reference standards<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

The consequence is unambiguous.<\/strong> The study results cited further on this page were obtained exclusively using the registered medicinal product<\/strong> (salt form, clinical trials in humans) or concern the acid form itself in a purely analytical context<\/strong> — methods for its determination, not its effects. None of the cited clinical studies were conducted using the analytical reagent<\/strong>, and none of these results carry over to the material offered here. The reagent is not the form in which the substance was ever administered to humans, and it cannot be used in that way.<\/p>\n

Reagent Identification Card<\/h2>\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Registry data and identifiers — tianeptine, acid form<\/caption>\n
Systematic name (IUPAC)<\/th>\n7-{[3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl]amino}heptanoic acid<\/td>\n<\/tr>\n
Common name<\/th>\ntianeptine, acid form (tianeptine acid)<\/td>\n<\/tr>\n
CAS Number<\/th>\n66981-73-5<\/td>\n<\/tr>\n
Molecular formula<\/th>\nC21<\/sub>H25<\/sub>ClN2<\/sub>O4<\/sub>S<\/td>\n<\/tr>\n
Molar mass<\/th>\n436.95 g·mol−1<\/sup><\/td>\n<\/tr>\n
Monoisotopic mass<\/th>\n436.1224 Da<\/td>\n<\/tr>\n
InChIKey<\/th>\nJICJBGPOMZQUBB-UHFFFAOYSA-N<\/td>\n<\/tr>\n
SMILES<\/th>\nCN1C2=CC=CC=C2C(C3=C(S1(=O)=O)C=C(C=C3)Cl)NCCCCCCC(=O)O<\/td>\n<\/tr>\n
PubChem CID<\/th>\n68870<\/a><\/td>\n<\/tr>\n
ChEMBL<\/th>\nCHEMBL3644322<\/td>\n<\/tr>\n
Form<\/th>\ncrystalline powder, white to off-white<\/td>\n<\/tr>\n
Purity<\/th>\n≥ 99.41%<\/td>\n<\/tr>\n
Intended use<\/th>\nresearch reagent — not for consumption by humans or animals<\/strong><\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

Molecular Lineage: The French Tradition of Tricyclic Antidepressants<\/h2>\n

Tianeptine was developed in the laboratories of the French pharmaceutical company Servier as a modification of the classic tricyclic drug core. In place of the central ring typical of this class, a dibenzothiazepine system in 5,5-dioxide form<\/strong> was introduced — a seven-membered ring bearing a sulfone group oxidized to its maximum degree — and a methyl substituent together with a side chain terminating in a carboxyl group were attached to the ring nitrogen atom. It is precisely this seven-carbon heptanoic acid chain<\/strong> that distinguishes the entire tianeptine family from other tricyclic psychotropic compounds and gives it physicochemical properties unusual for this class.<\/p>\n

Place Within the Tricyclic Drug Family<\/h3>\n

Classic tricyclic antidepressants (amitriptyline, imipramine) have a dibenzazepine or dibenzocycloheptane core and a short, simple side chain. The tianeptine core is structurally related, but the presence of sulfur at the sulfone oxidation state and the extended, acid-terminated chain mean the compound is sometimes described as atypical<\/strong> within this class — a description that concerns the chemical structure and the historically studied pharmacological profile of the registered drug, not the properties of the reagent offered here [7<\/a>].<\/p>\n

The Role of Chance in the Discovery of Antidepressants<\/h3>\n

The history of antidepressant pharmacology — from imipramine to atypical derivatives — is largely a history of observing the side effects of compounds under study, rather than deliberate design from the ground up. This phenomenon, described as the role of serendipity in pharmaceutical discovery, was systematized in a recent historical analysis based on operational criteria covering the development of successive generations of this drug class [11<\/a>]. An early French clinical review from 1989 described tianeptine outright as an "uncommon psychotropic drug"<\/em> — a phrase that referred to the preparation registered at the time, not to the free acid as a laboratory material [3<\/a>].<\/p>\n

Timeline<\/h2>\n\n\n\n\n\n\n\n\n\n\n\n\n
Timeline: molecule origin and development of the pharmacokinetic literature<\/caption>\n
1970s–1980s<\/th>\nmolecule developed in the laboratories of the Servier concern (France) as a modification of the tricyclic antidepressant core<\/td>\n<\/tr>\n
1986<\/th>\nfirst published ion-pair extraction and HPLC method for determining tianeptine and its metabolites in plasma, urine, and tissues [1<\/a>]<\/td>\n<\/tr>\n
1988<\/th>\nstudy of the effect of food on the absorption kinetics of the registered preparation, University of Liege [2<\/a>]<\/td>\n<\/tr>\n
1989<\/th>\nFrench clinical review [3<\/a>]; concurrently, pharmacokinetics in patients with chronic alcoholism and cirrhosis, Nancy hospital [4<\/a>]<\/td>\n<\/tr>\n
1990<\/th>\ntwo papers from the manufacturer’s own research institute: disposition in renal failure and during hemodialysis [5<\/a>] and the effect of concurrent alcohol administration in healthy volunteers [6<\/a>]<\/td>\n<\/tr>\n
2008<\/th>\ncomprehensive review of the neurobiology and clinical effects of the registered drug [7<\/a>]<\/td>\n<\/tr>\n
2018<\/th>\nreview of 18 case reports of abuse and dependence in the psychiatric literature [8<\/a>]<\/td>\n<\/tr>\n
2019<\/th>\nreview of the atypical pharmacological mechanism of the registered drug [9<\/a>]<\/td>\n<\/tr>\n
2022<\/th>\nretrospective identification of novel psychoactive substances in clinical samples using analytical methods, including tianeptine [10<\/a>]<\/td>\n<\/tr>\n
2025<\/th>\nhistorical analysis of the role of chance in antidepressant discovery [11<\/a>]; review of antidepressant interactions with the endogenous opioid system [12<\/a>]<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

Three Institutional Sources of Early Pharmacokinetics<\/h2>\n

The early pharmacokinetic literature on the registered drug has a clear, documented institutional geography — some work originated at the manufacturer's own research institute, some at independent academic centers:<\/p>\n