GSK-588045
A selective serotonin receptor antagonist
| GSK-588045 | |
|---|---|
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| INN | |
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| CAS Number | 957135-43-2 |
| PubChem | 11550036 |
| DrugBank | |
| ChemSpider | 9720480 |
| KEGG | |
GSK-588045 is a chemical compound that acts as a selective antagonist of the 5-HT6 receptor, a subtype of the serotonin receptor. It was developed by GlaxoSmithKline for potential use in the treatment of cognitive disorders such as Alzheimer's disease and schizophrenia.
Pharmacology[edit | edit source]
GSK-588045 is known for its high affinity and selectivity for the 5-HT6 receptor, which is predominantly expressed in the central nervous system. The 5-HT6 receptor is involved in the modulation of neurotransmitter release, including acetylcholine, dopamine, and glutamate, which are critical for cognitive processes. By antagonizing this receptor, GSK-588045 may enhance cognitive function and has been investigated for its potential benefits in neurodegenerative and psychiatric conditions.
Mechanism of Action[edit | edit source]
The mechanism of action of GSK-588045 involves the blockade of the 5-HT6 receptor, which leads to increased release of neurotransmitters that are important for learning and memory. This receptor is a G protein-coupled receptor that, when activated, can inhibit the release of these neurotransmitters. By blocking the receptor, GSK-588045 may facilitate neurotransmitter release and improve cognitive function.
Development and Research[edit | edit source]
Research into GSK-588045 has focused on its potential therapeutic effects in conditions characterized by cognitive deficits. Preclinical studies have shown promising results in animal models, where the compound improved performance in tasks that require learning and memory. However, the development of GSK-588045 for clinical use has been limited, and it remains primarily a research compound.
Potential Applications[edit | edit source]
The potential applications of GSK-588045 include the treatment of cognitive impairments associated with Alzheimer's disease, schizophrenia, and other neuropsychiatric disorders. By improving cognitive function, it could help alleviate some of the symptoms associated with these conditions, although further research is needed to confirm its efficacy and safety in humans.
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Contributors: Prab R. Tumpati, MD
