Ro48-6791
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Ro48-6791 is a drug, an imidazo
benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...
derivative developed by
Hoffman-LaRoche F. Hoffmann-La Roche AG, commonly known as Roche, is a Swiss multinational healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX S ...
in the 1990s. Ro48-6791 was developed as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Ro48-6791 has properties similar to those of midazolam, being water-soluble, with a fast onset and short duration of action. It is 4-6x more potent than midazolam, and slightly shorter acting, and produces similar side effects such as sedation and amnesia. It was tested up to Phase II human trials, but while it produced less
respiratory depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapnia ...
than
propofol Propofol, marketed as Diprivan, among other names, is a short-acting medication that results in a decreased level of consciousness and a lack of memory for events. Its uses include the starting and maintenance of general anesthesia, sedation f ...
, it had a longer recovery time and was deemed not to have any significant advantages over the older drug. Similarly when Ro48-6791 was compared to midazolam, it had similar efficacy, higher potency and a shorter recovery time, but produced less of a synergistic effect on opioid-induced analgesia and produced more severe side effects such as dizziness after the procedure. Consequently, it was dropped from clinical development, although it is still used in scientific research.


See also

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Benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...


References

{{GABAAR PAMs GABAA receptor positive allosteric modulators Drugs developed by Hoffmann-La Roche Imidazobenzodiazepines Lactams Fluoroarenes Oxadiazoles