SB-271,046

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SB-271046_structure.png



SB-271,046 is a chemical compound that acts as a potent and selective antagonist for the 5-HT6 receptor. It was developed by the pharmaceutical company GlaxoSmithKline and has been used extensively in scientific research to investigate the role of the 5-HT6 receptor in the central nervous system.

Pharmacology[edit | edit source]

SB-271,046 is known for its high affinity and selectivity for the 5-HT6 receptor, a subtype of the serotonin receptor family. The 5-HT6 receptor is predominantly expressed in the brain, particularly in regions such as the cortex, hippocampus, and striatum. These areas are associated with cognitive processes, including learning and memory.

Mechanism of Action[edit | edit source]

As an antagonist, SB-271,046 binds to the 5-HT6 receptor and inhibits its activity. This blockade can modulate the release of various neurotransmitters, including acetylcholine, dopamine, and glutamate, which are crucial for cognitive functions. The precise mechanism by which SB-271,046 enhances cognitive performance is still under investigation, but it is believed to involve the modulation of these neurotransmitter systems.

Research and Applications[edit | edit source]

SB-271,046 has been used in numerous preclinical studies to explore the potential therapeutic benefits of 5-HT6 receptor antagonists. Research has suggested that SB-271,046 may improve cognitive deficits in animal models of Alzheimer's disease and schizophrenia.

Cognitive Enhancement[edit | edit source]

Studies have shown that SB-271,046 can enhance performance in various cognitive tasks, such as the Morris water maze and novel object recognition test. These findings suggest that 5-HT6 receptor antagonists like SB-271,046 could be potential candidates for the treatment of cognitive disorders.

Potential Therapeutic Uses[edit | edit source]

While SB-271,046 itself has not been developed as a therapeutic drug, its role in research has paved the way for the development of other 5-HT6 receptor antagonists that are currently being investigated in clinical trials for conditions such as Alzheimer's disease and attention deficit hyperactivity disorder (ADHD).

Safety and Toxicology[edit | edit source]

The safety profile of SB-271,046 has been evaluated in preclinical studies. While it is generally well-tolerated in animal models, further research is needed to fully understand its safety and efficacy in humans.

Also see[edit | edit source]

Template:Receptor pharmacology

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Contributors: Prab R. Tumpati, MD