Related Experiment Video
Updated: Jun 11, 2025
10:53
Preparation of Acute Brain Slices Using an Optimized N-Methyl-D-glucamine Protective Recovery Method
Published on: February 26, 2018
46.1K
Classics in Chemical Neuroscience: Tianeptine
ACS Chemical Neuroscience
|October 9, 2024
Summary
Tianeptine, an antidepressant, acts on opioid receptors, not serotonin pathways. Its mu-opioid receptor agonism contributes to a growing potential for recreational abuse and global regulatory scrutiny.
Area of Science:
- Neuroscience
- Pharmacology
- Medicinal Chemistry
Background:
- Tianeptine is an atypical antidepressant with a unique mechanism of action.
- Its efficacy is not linked to serotonin receptors or monoamine transporters.
- Tianeptine exhibits agonist activity at mu-opioid receptors (MOR) and delta-opioid receptors (DOR).
Purpose of the Study:
- To review the medicinal chemistry and pharmacology of tianeptine.
- To explore the discrepancy between its therapeutic use and emerging abuse potential.
- To discuss the implications of its mu-opioid receptor activity.
Main Methods:
- Literature review of pharmacological studies.
- Analysis of case reports on tianeptine use.
- Examination of neuroplasticity pathways involving glutamate.
Main Results:
- Tianeptine's antidepressant effects may involve glutamate pathways.
- Significant mu-opioid receptor agonism is identified as a key pharmacological property.
- Increasing reports indicate recreational misuse of tianeptine at high doses.
Conclusions:
- Tianeptine's mu-opioid receptor activity presents a significant liability for abuse.
- Regulatory actions, including bans and reclassifications, are increasing globally.
- The dual profile of tianeptine necessitates careful consideration of its risks and benefits.
More Related Videos
11:44Cellular Membrane Affinity Chromatography Columns to Identify Specialized Plant Metabolites Interacting with Immobilized Tropomyosin Kinase Receptor B
Published on: January 19, 2022
2.5K
10:20Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
8.5K
Related Concept Videos
01:26Neurochemical Transmission: Sites of Drug Action
2.1K
Neurochemical transmission, the conduction of electrical impulses between neurons mediated by neurotransmitters, plays a vital role in various physiological processes. Autonomic drugs exert their effects by modulating neurotransmission within the autonomic nervous system. For instance, drugs such as hemicholinium block the precursor uptake necessary for synthesizing acetylcholine, an essential autonomic neurotransmitter. Following synthesis, neurotransmitters are stored in vesicles. Metyrosine...
2.1K
01:24Resting Membrane Potential
18.1K
The relative difference in electrical charge, or voltage, between the inside and the outside of a cell membrane, is called the membrane potential. It is generated by differences in permeability of the membrane to various ions and the concentrations of these ions across the membrane.
The Inside of a Neuron is More Negative
The membrane potential of a cell can be measured by inserting a microelectrode into a cell and comparing the charge to a reference electrode in the extracellular fluid. The...
The Inside of a Neuron is More Negative
The membrane potential of a cell can be measured by inserting a microelectrode into a cell and comparing the charge to a reference electrode in the extracellular fluid. The...
18.1K
01:30Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.1K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.1K
01:21Drugs Affecting Neurotransmitter Release or Uptake
970
Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
970
01:26Chemical Synapses
8.7K
Chemical synapses are specialized sites between two neurons or between a neuron and a non-neuronal cell like a muscle, glandular or sensory cell.
Because chemical synapses depend on the release of neurotransmitter molecules from synaptic vesicles to pass on their signal, there is an approximately one millisecond delay between when the axon potential reaches the presynaptic terminal and when the neurotransmitter leads to opening of postsynaptic ion channels. Additionally, this signaling is...
Because chemical synapses depend on the release of neurotransmitter molecules from synaptic vesicles to pass on their signal, there is an approximately one millisecond delay between when the axon potential reaches the presynaptic terminal and when the neurotransmitter leads to opening of postsynaptic ion channels. Additionally, this signaling is...
8.7K
01:20Desensitization and Tachyphylaxis
1.6K
Tachyphylaxis is described as a rapid decrease in response to a drug after repeated or continuous administration of the same drug dose. It is a phenomenon where the body becomes less responsive to a particular substance or intervention over time, requiring higher doses or stronger interventions to achieve the same effect. It results from adaptive changes in the body's receptors, signaling pathways, or physiological processes that occur in response to prolonged exposure to a stimulus.
1.6K