beta-Funaltrexamine (beta-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible µ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. beta-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking µ-opioid receptors, and reduces the transcriptional activities of NF-kappaB, AP-1, CREB and Stat. Furthermore, beta-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. beta-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases[1][2][3][4].
