SB-656104

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SB-656104 is a chemical compound that acts as a selective antagonist for the 5-HT7 receptor, a subtype of the serotonin receptor family. It was developed by GlaxoSmithKline for research purposes and has been used in various studies to explore the role of the 5-HT7 receptor in the central nervous system.

Pharmacology

SB-656104 is known for its high affinity and selectivity for the 5-HT7 receptor, which is involved in the regulation of mood, circadian rhythm, and cognitive functions. By blocking this receptor, SB-656104 can help elucidate the physiological and pathological roles of 5-HT7 in various conditions, including depression, anxiety, and schizophrenia.

Mechanism of Action

The 5-HT7 receptor is a G protein-coupled receptor (GPCR) that, when activated by serotonin, can influence the production of cyclic AMP (cAMP) in neurons. SB-656104 binds to the 5-HT7 receptor and prevents serotonin from activating it, thereby inhibiting the downstream signaling pathways that would normally be triggered by receptor activation.

Research Applications

SB-656104 has been used extensively in preclinical studies to investigate the role of the 5-HT7 receptor in various neurological and psychiatric disorders. For example, studies have shown that SB-656104 can modulate sleep patterns and improve cognitive deficits in animal models, suggesting potential therapeutic applications for sleep disorders and cognitive impairments.

Safety and Toxicology

As a research compound, SB-656104 has not been approved for clinical use in humans. Its safety profile has been primarily evaluated in animal studies, where it has shown a relatively low toxicity at doses used for research purposes. However, comprehensive toxicological data in humans are lacking.

Also see

• 5-HT7 receptor
• Serotonin receptor
• GlaxoSmithKline
• Antagonist (pharmacology)
• Neurotransmitter