Estianeptine
Pharmaceutical compound
From Wikipedia, the free encyclopedia
Estianeptine, also known as (S)-tianeptine and by its developmental code name TNX-4300, is a peroxisome proliferator-activated receptor (PPAR) agonist and atypical tricyclic antidepressant (TCA) which is under development for the treatment of Alzheimer's disease, bipolar disorders, major depressive disorder, and Parkinson's disease.[1][2][3][4][5] It is taken orally.[1]
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| Other names | (S)-Tianeptine; S-Tianeptine; TNX-4300; TNX4300 |
| Routes of administration | Oral[1] |
| Drug class | Peroxisome proliferator-activated receptor (PPAR) agonist; PPARβ/δ and PPARγ agonist |
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| Formula | C21H25ClN2O4S |
| Molar mass | 436.95 g·mol−1 |
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Pharmacology
Estianeptine is the (S)- enantiomer of the atypical tricyclic antidepressant (TCA) and weak opioid tianeptine.[1][4][5][6] It acts as a selective PPARβ/δ and PPARγ agonist.[1][2][4][7] The drug has been found to promote neuroplasticity in vitro, which is thought to be mediated by its PPAR agonism.[4][7] In addition, it has been found to improve cognition and memory in rodents.[8][9] In contrast to tianeptine and (R)-tianeptine, estianeptine shows no activity as a μ-opioid receptor (MOR) agonist.[1][4][7] Moreover, unlike estianeptine, (R)-tianeptine has no activity as a PPAR agonist.[4][7] It has been proposed that estianeptine, via its PPAR agonism, is responsible for the antidepressant effects of tianeptine, rather than tianeptine's weak MOR agonism that manifests at high doses being responsible.[4][7][10] Tianeptine's PPAR agonism may also be responsible for the drug's anti-inflammatory effects.[7]
History
Estianeptine was first described in the scientific literature by 1997.[11] It is being developed by Tonix Pharmaceuticals.[1][2][4] As of August 2023, the drug is in the preclinical research stage of development for all indications.[1][2] Tianeptine's PPAR agonism was first described in 2022.[12]