In vitro and in vivo pharmacological characterization of fentanyl analogs.

ABSTRACT: Opioid overdose is the leading cause of unintentional drug-related deaths in the United States (US), largely due to the use of illicitly manufactured synthetic opioids like fentanyl and its analogs. The pharmacological properties of novel fentanyl analogs are largely unknown. Thus, this study characterized opioid-like activities of six novel fentanyl analogs (acryl fentanyl, β-hydroxythio fentanyl, cyclohexyl fentanyl, 4-fluoroisobutyrly fentanyl, furanyl fentanyl, and tetrahydrofuranyl fentanyl) in vitro and in vivo, in comparison to morphine and fentanyl. In radioligand binding assays using [³H](D-Ala², N-MePhe⁴, Gly-ol)-enkephalin (DAMGO) and the human mu opioid receptor (MOR) stably expressed in Chinese hamster ovary cells, all test substances except cy

SUBMITTER: Obeng S 

PROVIDER: S-EPMC12408109 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature