Related Experiment Video
Updated: Dec 20, 2025
10:53
Preparation of Acute Brain Slices Using an Optimized N-Methyl-D-glucamine Protective Recovery Method
Published on: February 26, 2018
48.1K
Classics in Chemical Neuroscience: Baclofen.
Caitlin N Kent1,2, Charlotte Park1, Craig W Lindsley1,3,2,4
1Warren Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.
ACS Chemical Neuroscience
|May 22, 2020
Summary
Baclofen is the only FDA-approved GABAB agonist, initially for spasticity. This review explores its history, pharmacology, and societal impact, including off-label uses for addiction treatment.
Area of Science:
- Neuroscience
- Pharmacology
- Chemical Neuroscience
Background:
- Baclofen is the sole FDA-approved GABAB agonist, developed as a brain-penetrant analog of GABA.
- Initially investigated for epilepsy, its potent muscle relaxant properties led to approval for spasticity treatment.
- Baclofen's FDA approval preceded the discovery of its receptor and full elucidation of its mechanism of action.
Purpose of the Study:
- To provide a comprehensive review of baclofen's >60-year legacy.
- To detail the history, pharmacology, synthesis, metabolism, and administration of baclofen.
- To examine the societal impact and off-label applications of baclofen, particularly in addiction treatment.
Main Methods:
- Literature review of baclofen's historical development and scientific literature.
- Analysis of pharmacological data, including receptor interactions and mechanism of action.
- Examination of clinical applications, including approved and off-label uses.
Main Results:
- Baclofen's unique position as the only FDA-approved GABAB agonist is highlighted.
- Its efficacy in treating spasticity is well-established, stemming from its muscle relaxant properties.
- Emerging off-label uses, especially for alcohol and drug addiction, show significant therapeutic potential.
Conclusions:
- Baclofen remains a significant compound in chemical neuroscience with a rich history.
- Its multifaceted applications continue to expand beyond its initial indications.
- Further research into baclofen's mechanisms and applications holds promise for various neurological conditions and substance abuse disorders.
More Related Videos
Related Concept Videos
01:29Spasmolytic Agents: Chemical Classification
1.2K
Spasmolytic agents are drugs used to alleviate muscle spasms and spasticity. They can be categorized into different chemical groups based on their mechanisms of action. Centrally acting spasmolytics primarily affect the spinal cord, while others directly target skeletal muscle cells.
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also...
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also...
1.2K
01:29Drug Delivery: Parenteral Route
1.3K
The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
1.3K
01:28Classification of Skeletal Muscle Relaxants
2.9K
Skeletal muscle relaxants are a group of drugs that can reduce muscle stiffness and induce temporary paralysis to relieve pain. These agents can act centrally to reduce muscle tone or spasms in painful conditions such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), or spinal injuries; they are called antispasmodics or spasmolytics.
Peripherally acting skeletal muscle relaxants interfere with the neurotransmission at the neuromuscular end plate to induce paralysis during...
Peripherally acting skeletal muscle relaxants interfere with the neurotransmission at the neuromuscular end plate to induce paralysis during...
2.9K
01:26Chemical Synapses
11.0K
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...
11.0K
01:26Chemical Synapses
4.0K
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...
4.0K
01:26Neurochemical Transmission: Sites of Drug Action
3.3K
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...
3.3K