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Nalorphine is a mixed opioid agonist–antagonist that was introduced in 1954. It acts as an antagonist at the mu-opioid receptor and as a high-efficacy agonist at the kappa-opioid receptor. Its primary historical uses were to reverse opioid overdose and in challenge tests to determine opioid dependence. While it has some analgesic properties, its potent activation of the kappa-opioid receptor leads to side effects such as dysphoria, anxiety, confusion, and hallucinations, making it unsuitable for routine medical use today. Nalorphine has largely been replaced by pure antagonists like naloxone for clinical applications[1][2][3][5].
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