Oliceridine (also known as TRV130) is a G-protein-biased
ligand at the μ-opioid receptor. In
preclinical studies, it was potently analgesic while causing less respiratory
depression and gastrointestinal dysfunction than morphine, suggesting unique
benefits in acute pain management. This unique “G protein-biased” μ-opioid ligand is a
potent analgesic in rodents, with 3-10 times the potency of morphine, but with
reduced gastrointestinal (GI) dysfunction and respiratory depression compared
to equianalgesic doses of morphine.
The margin between Oliceridine analgesia and side effects (therapeutic index) in rodents suggests that Oliceridine may be a safer, tolerable analgesic than current parenterally administered opioids such as morphine, fentanyl, and hydromorphone. It is currently in Phase-III trials.
For more details, order the pdf by sending an email at sharma.rajan@gmail.com. Report has all the features that this site has provided to its users such as structure, synthesis, and activity results.
For more details, order the pdf by sending an email at sharma.rajan@gmail.com. Report has all the features that this site has provided to its users such as structure, synthesis, and activity results.
