VU-0152100
VU-0152100 is a chemical compound that acts as a selective positive allosteric modulator of the metabotropic glutamate receptor subtype mGluR4. It is primarily used in scientific research to study the role of mGluR4 in the central nervous system and its potential therapeutic applications.
Mechanism of Action[edit | edit source]
VU-0152100 functions by binding to an allosteric site on the mGluR4 receptor, which is distinct from the orthosteric site where the endogenous ligand, glutamate, binds. This binding enhances the receptor's response to glutamate, thereby modulating neurotransmission. The mGluR4 receptor is a G-protein coupled receptor (GPCR) that is involved in the regulation of neurotransmitter release in the brain.
Pharmacological Effects[edit | edit source]
The activation of mGluR4 by VU-0152100 has been shown to have several effects in preclinical models:
- Neuroprotection: VU-0152100 has demonstrated neuroprotective effects in models of Parkinson's disease, suggesting its potential as a therapeutic agent for neurodegenerative disorders.
- Analgesia: Modulation of mGluR4 has been associated with analgesic effects, indicating a possible role in pain management.
- Anxiolytic Effects: Studies have shown that VU-0152100 may reduce anxiety-like behaviors, which could be beneficial in treating anxiety disorders.
Research Applications[edit | edit source]
VU-0152100 is used extensively in research to explore the therapeutic potential of mGluR4 modulation. It serves as a tool compound to:
- Investigate the role of mGluR4 in various neurological and psychiatric disorders.
- Develop new therapeutic strategies targeting mGluR4 for conditions such as schizophrenia, anxiety disorders, and chronic pain.
Safety and Toxicology[edit | edit source]
As a research compound, VU-0152100 is not approved for clinical use in humans. Its safety profile is primarily characterized in animal studies, where it has shown a favorable safety margin. However, further studies are required to fully understand its toxicological properties.
Also see[edit | edit source]
- Metabotropic glutamate receptor
- Allosteric modulator
- Neurotransmission
- Parkinson's disease
- G-protein coupled receptor
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Contributors: Prab R. Tumpati, MD