beta-funaltrexamine

beta-Funaltrexamine (beta-FNA) is a highly selective and irreversible antagonist of the mu-opioid receptor (MOR). Derived from naltrexone, it contains an electrophilic fumarate methyl ester group that allows it to form a covalent bond with the receptor, leading to long-lasting blockade. While it acts as an irreversible antagonist at the mu-receptor, it also exhibits reversible agonist activity at the kappa-opioid receptor (KOR). beta-FNA is widely utilized as a pharmacological tool in neuroscience and pain research to differentiate between opioid receptor subtypes and to study the long-term effects of mu-receptor inactivation. In research settings, it has also been studied for its effects on opioid receptor expression and cell proliferation in various cell lines, including MCF-7 breast cancer cells.

Other names

beta-funaltrexamine hydrochloriden-((E)-4-(bis(2-chloroethyl)amino)-2-butenyl)naltrexone