Abstract
Developing non-addictive and safer opioids for pain management is unmet medical need. Among a number of bioreversible derivatives of Nalbuphine – an equipotent to morphine opioid without serious side effects - NB-33 was identified in silico and confirmed in vivo as a superior analgesic agent. Apart from enhanced pharmacodynamics profile, NB-33 outperformed the parent compound on equimolar bases in cold ethanol tail-flick and mechanical models of pain in rats. With no β-arrestin engagement liability, good stability in simulated gastro-intestinal fluid and slow release of Nalbuphine by plasma NB-33 is being developed as an oral and safer alternative of its parent drug.
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