Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor ( IC 50 =50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor ( OPRK ) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor ( OPRM ) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals , and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity.
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