Ro 19-4603

Ro 19-4603 is an inverse agonist of the benzodiazepine binding site. It has effects antagonistic to those of benzodiazepines.

Chemistry
Despite acting at the benzodiazepine site, it does not possess the benzodiazepine structure. It is an Imidazothienodiazepine: a thiophene ring, an imidazole ring and a diazepine ring fused together.

Effects & Pharmacodynamics
Ro 19-4603 is an inverse agonist at the benzodiazepine binding site. Due to this, it has effects similar to other benzodiazepine inverse agonists, notably: anxiogenesis, convulsions.

Administration of this compound was able to decrease voluntary alcohol consumption. This was also observed in rats selected for high alcohol preference. In addition to decreasing its consumption, Ro 19-4603 is able to antagonize the intoxicating effects of alcohol.