Naloxone is a μ-opioid receptor (MOR) inverse agonist. Naloxone has an extremely high affinity for μ-opioid receptors in the central nervous system (CNS). Its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- (KOR) and δ-opioid receptors (DOR). The mechanism of action is not completely understood, but studies suggest it functions to produce withdrawal symptoms by competing for opiate receptor sites within the CNS (a competitive antagonist, not a direct agonist), thereby preventing the action of both endogenous and xenobiotic opiates on these receptors without directly producing any effects itself. Naloxone was approved for opioid overdose by the Food and Drug Administration in 1971. References: McDonald R, Strang J. Are take-home naloxone programmes effective? Systematic review utilizing application of the Bradford Hill criteria. Addiction. 2016 Mar 30. doi: 10.1111/add.13326. [Epub ahead of print] Review. PubMed PMID: 27028542.

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CAS：465-65-6