SB-408124

SB-408124 is a drug that acts as a selective antagonist for the Orexin receptor OX1, with around 50x selectivity for OX1 over the related OX2 receptor. It has been used in scientific research to explore the role of the orexin system in various processes, and has been shown to produce anxiolytic effects in animal studies.

Pharmacology

SB-408124 is a potent and selective non-peptide antagonist of OX1 Orexin receptor. It has a high affinity for the OX1 receptor, with a Ki of 40 nM, and over 50 times selectivity over the OX2 receptor. This selectivity makes it a useful tool in the study of the orexin system, as it allows the effects of OX1 activation to be studied in isolation.

Uses in Research

SB-408124 has been used in a variety of research contexts to investigate the role of the orexin system in various physiological and pathological processes. These include studies on sleep regulation, feeding behavior, stress response, and drug addiction. In particular, it has been used to investigate the role of the OX1 receptor in the regulation of sleep and wakefulness, and in the response to stress and addictive drugs.

Clinical Significance

The orexin system, and the OX1 receptor in particular, has been implicated in a number of clinical conditions, including insomnia, narcolepsy, obesity, and drug addiction. As a result, drugs that modulate the activity of this system, such as SB-408124, may have potential therapeutic applications. However, further research is needed to fully understand the role of the orexin system in these conditions and to develop effective treatments.

See Also

• Orexin receptor
• Orexin
• Orexin antagonist

References

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