R-tianeptine

R-tianeptine is the (R)-enantiomer of the atypical antidepressant tianeptine. While the racemic form of tianeptine has been used clinically for decades, R-tianeptine is being developed as a standalone candidate, most notably by Tonix Pharmaceuticals as TNX-601R. Its primary mechanism of action involves full agonism at the mu-opioid receptor (MOR). This activation is thought to trigger downstream modulation of the glutamatergic system, including the enhancement of AMPA receptor signaling and the normalization of NMDA receptor-mediated neurotransmission. These effects promote neuroplasticity and reverse stress-induced dendritic atrophy in the hippocampus and prefrontal cortex. R-tianeptine has been investigated for Major Depressive Disorder (MDD), Post-Traumatic Stress Disorder (PTSD), and neurocognitive dysfunction, though recent Phase 2 trials in MDD failed to meet their primary endpoints.

Other names

(R)-tianeptine(+)-tianeptineR-(+)-tianeptine