SB-649868

SB-649868 is a drug that was developed by GlaxoSmithKline for the treatment of insomnia and other sleep disorders. It is a dual orexin receptor antagonist, which means it blocks the action of the neurotransmitters orexin A and orexin B. These neurotransmitters are involved in the regulation of sleep-wake cycle, appetite, and arousal.

History

SB-649868 was first synthesized by GlaxoSmithKline in the early 2000s as part of their research into the role of orexins in sleep disorders. The drug entered clinical trials in 2005, but development was discontinued in 2011 for undisclosed reasons.

Mechanism of action

SB-649868 works by blocking the action of the neurotransmitters orexin A and orexin B at their receptors, OX1R and OX2R. These neurotransmitters are produced by neurons in the hypothalamus, a region of the brain that plays a key role in regulating sleep and wakefulness. By blocking the action of orexins, SB-649868 promotes sleep and reduces wakefulness.

Clinical trials

In clinical trials, SB-649868 was found to be effective in reducing insomnia symptoms and improving sleep quality. However, some participants experienced side effects such as headache, dizziness, and nausea. The drug was not approved for use by any regulatory authority, and development was discontinued in 2011.

Potential uses

Despite the discontinuation of its development, SB-649868 has been the subject of ongoing research due to its potential uses in treating other conditions. These include narcolepsy, a sleep disorder characterized by excessive daytime sleepiness and sudden attacks of sleep, and Parkinson's disease, a neurodegenerative disorder that can cause sleep disturbances.

See also

• Orexin receptor antagonist
• Sleep disorders
• Insomnia