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- Tianeptine is a unique antidepressant that works differently from traditional ones, as it doesn't mainly affect serotonin receptors or monoamine transporters.
- It has been found to act as an agonist on mu and delta opioid receptors, and its effectiveness might be linked to changes in glutamate signaling and neuroplasticity.
- There is growing concern about its potential for abuse, with reports of recreational use at high doses, leading some regions to consider stricter regulations or bans on its availability.
Activation of μ receptors by SR-17018 through a distinctive mechanism.
Neuropharmacology
November 2024
Institute of Academic Anaesthesia, Division of Systems Medicine, School of Medicine, Ninewells Hospital, University of Dundee, Dundee, DD1 9SY, UK. Electronic address:
Agonists at μ opioid receptors relieve acute pain, however, their long-term use is limited by side effects, which may involve β-arrestin2. Agonists biased against β-arrestin2 recruitment may be advantageous. However, the classification of bias may be compromised by assays utilising overexpressed μ receptors which overestimate efficacy for G-protein activation.
View Article and Find Full Text PDFAssessment of the potential of novel and classical opioids to induce respiratory depression in mice.
Br J Pharmacol
December 2023
Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, Queen's Medical Centre, University of Nottingham, Nottingham, UK.
Background And Purpose: Opioid-induced respiratory depression limits the use of μ-opioid receptor agonists in clinical settings and is the main cause of opioid overdose fatalities. The relative potential of different opioid agonists to induce respiratory depression at doses exceeding those producing analgesia is understudied despite its relevance to assessments of opioid safety. Here we evaluated the respiratory depressant and anti-nociceptive effects of three novel opioids and relate these measurements to their in vitro efficacy.
View Article and Find Full Text PDFTianeptine promotes lasting antiallodynic effects in a mouse model of neuropathic pain.
Neuropsychopharmacology
October 2023
Nash Family Department of Neuroscience, Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.
Tricyclic antidepressants (TCAs), such as desipramine (DMI), are effective at managing neuropathic pain symptoms but often take several weeks to become effective and also lead to considerable side effects. Tianeptine (TIAN) is an atypical antidepressant that activates the mu-opioid receptor but does not produce analgesic tolerance or withdrawal in mice, nor euphoria in humans, at clinically-relevant doses. Here, we evaluate the efficacy of TIAN at persistently alleviating mechanical allodynia in the spared nerve injury (SNI) model of neuropathic pain, even well after drug clearance.
View Article and Find Full Text PDFRole of efficacy as a determinant of locomotor activation by mu-opioid receptor (MOR) ligands in female and male mice. II. Effects of novel MOR-selective phenylmorphans with high-to-low MOR efficacy.
Pharmacol Res Perspect
August 2023
Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, Virginia, USA.
Low-efficacy mu-opioid receptor (MOR) agonists represent promising therapeutics, but existing compounds (e.g., buprenorphine, nalbuphine) span a limited range of low MOR efficacies and have poor MOR selectivity.
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