Ro15-4513

Ro15-4513

Ro15-4513 is a pharmacological compound that is classified as an inverse agonist of the benzodiazepine receptor. It was first synthesized by the pharmaceutical company Hoffmann-La Roche in the 1980s. Ro15-4513 is particularly notable for its ability to counteract the effects of ethanol (alcohol), and has been the subject of extensive research in this context.

Chemistry

Ro15-4513 is a derivative of the benzodiazepine class of drugs, but unlike most benzodiazepines, it is an inverse agonist rather than an agonist. This means that it binds to the same receptor sites as benzodiazepines, but induces the opposite effect. The chemical structure of Ro15-4513 includes a furan ring, which is not present in most other benzodiazepines.

Pharmacology

Ro15-4513 acts primarily on the GABA_A receptor, the same receptor targeted by benzodiazepines. However, while benzodiazepines enhance the effect of the neurotransmitter GABA at this receptor, leading to sedative and anxiolytic effects, Ro15-4513 reduces the effect of GABA, leading to increased alertness and potentially anxiety.

Research and potential applications

The most significant potential application of Ro15-4513 is in the treatment of alcohol intoxication and dependence. In animal studies, Ro15-4513 has been shown to counteract the sedative effects of alcohol, and it has been suggested that it could be used to rapidly reverse alcohol intoxication in emergency situations. However, the potential for anxiety-inducing side effects has limited its use in humans.

See also

• Benzodiazepine
• GABA_A receptor
• Inverse agonist
• Ethanol

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