Naloxazone

Naloxazone

Naloxazone is a derivative of naltrexone that is used in scientific research. It is a competitive antagonist for the mu opioid receptor, but has been shown to act as an inverse agonist at the kappa opioid receptor.

Chemistry

Naloxazone is a morphinan derivative and is structurally similar to other morphinan-based opioid antagonists such as naltrexone and naloxone. It is synthesized from thebaine, a constituent of opium.

Pharmacology

Naloxazone acts primarily as a competitive antagonist at the mu opioid receptor, which is the primary site of action for many opioid drugs. By binding to these receptors, naloxazone prevents opioids from exerting their analgesic effects. However, naloxazone has also been shown to act as an inverse agonist at the kappa opioid receptor. This means that it not only blocks the effects of kappa opioid agonists, but also produces effects that are opposite to those of kappa opioid agonists when administered alone.

Uses

Naloxazone is primarily used in scientific research. It is often used in studies investigating the role of the mu and kappa opioid receptors in pain, addiction, and other physiological processes.

Side Effects

As with other opioid antagonists, naloxazone can precipitate withdrawal symptoms in individuals who are physically dependent on opioids. Other potential side effects include nausea, vomiting, and increased pain sensitivity.

See Also

• Naltrexone
• Naloxone
• Opioid receptor
• Opioid antagonist