VU-0029767
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VU-0029767 is a chemical compound that acts as a selective positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4. It has been primarily used in scientific research to explore the role of M4 receptors in the central nervous system and their potential therapeutic applications.
Pharmacology
VU-0029767 enhances the activity of the M4 muscarinic receptor, which is a G protein-coupled receptor (GPCR) involved in various neurological processes. The M4 receptor is predominantly expressed in the striatum, a brain region associated with motor control and cognitive functions. By modulating this receptor, VU-0029767 can influence neurotransmitter release and neuronal excitability.
Mechanism of Action
As a positive allosteric modulator, VU-0029767 binds to a site on the M4 receptor distinct from the orthosteric site where the endogenous ligand, acetylcholine, binds. This binding enhances the receptor's response to acetylcholine, increasing its efficacy and potency. This mechanism allows for more precise modulation of receptor activity compared to direct agonists.
Research Applications
VU-0029767 has been utilized in preclinical studies to investigate the therapeutic potential of M4 receptor modulation in various neurological disorders, including schizophrenia, Parkinson's disease, and Alzheimer's disease. Its ability to modulate dopaminergic and cholinergic signaling pathways makes it a valuable tool in understanding the pathophysiology of these conditions.
Safety and Toxicology
While VU-0029767 has shown promise in research settings, its safety profile in humans has not been fully established. Preclinical studies in animal models are necessary to evaluate its potential side effects and toxicity before considering clinical trials.
Also see
- Muscarinic acetylcholine receptor
- Allosteric modulator
- G protein-coupled receptor
- Neurotransmitter
- Schizophrenia
- Parkinson's disease
- Alzheimer's disease
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Contributors: Prab R. Tumpati, MD
