Ro 15-4513

Ro 15-4513 is a pharmacological compound that belongs to the class of benzodiazepine derivatives. It was developed by the pharmaceutical company Hoffmann-La Roche in the 1980s. Ro 15-4513 is known for its unique ability to act as an inverse agonist at the GABA_A receptor, specifically at the ethanol binding site. This makes it a potential antidote for alcohol intoxication and a tool for studying alcohol addiction.

Pharmacology

Ro 15-4513 is a partial inverse agonist of the benzodiazepine receptor, which means it reduces the activity of the GABA_A receptor, the major inhibitory neurotransmitter receptor in the brain. Unlike most benzodiazepines, which enhance GABA_A receptor function and produce a sedative effect, Ro 15-4513 reduces GABA_A receptor function, which can lead to increased anxiety and seizures in animals.

Mechanism of Action

Ro 15-4513's unique mechanism of action involves binding to the ethanol site on the GABA_A receptor. This is a distinct site from the benzodiazepine binding site, and is thought to be responsible for some of the behavioral effects of alcohol. By binding to this site, Ro 15-4513 can block the effects of ethanol, making it a potential antidote for alcohol intoxication.

Research and Clinical Use

Ro 15-4513 has been used in research to study the effects of alcohol on the brain and the potential for new treatments for alcohol addiction. However, its use in humans is limited due to its potential to cause anxiety and seizures.

See Also

• Benzodiazepine
• GABA_A receptor
• Ethanol
• Hoffmann-La Roche