Ciproxifan

Ciproxifan is a histamine antagonist that has been primarily studied for its effects on wakefulness and alertness. It is a potent and selective H3 receptor antagonist with wake-promoting and cognitive-enhancing effects.

Pharmacology

Ciproxifan is a highly potent H3 antagonist, with a Ki of 9.63nM at the human H3 receptor, and over 1,000 times selectivity over the closely related H1, H2, and H4 receptors. It has been shown to increase histamine release in the brain, leading to increased wakefulness and alertness.

Clinical significance

Ciproxifan has been studied for its potential use in the treatment of narcolepsy and Alzheimer's disease, due to its ability to promote wakefulness and enhance cognition. However, it has not yet been approved for these uses.

See also

• Histamine H3 receptor
• Histamine antagonist

References

Ciproxifan Resources
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