Intranasal naloxone rapidly occupies brain mu-opioid receptors in human subjects.

ABSTRACT: Nasal spray formulations of naloxone, a mu-opioid receptor (MOR) antagonist, are currently used for the treatment of opioid overdose. They may have additional therapeutic utility also in the absence of opioid agonist drugs, but the onset and duration of action at brain MORs have been inadequately characterized to allow such projections. This study provides initial characterization of brain MOR availability at high temporal resolution following intranasal (IN) naloxone administration to healthy volunteers in the absence of a competing opioid agonist. Fourteen participants were scanned twice using positron emission tomography (PET) and [¹¹C]carfentanil, a selective MOR agonist radioligand. Concentrations of naloxone in plasma and MOR availability (relative to placebo) were monitor

SUBMITTER: Johansson J 

PROVIDER: S-EPMC6785104 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature