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Nicolas Milon

3 papers in the library · 60 citations · publishing 2015

Papers

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Noribogaine is a G-protein biased κ-opioid receptor agonist.

Neuropharmacology December 1, 2015 Émeline L. Maillet, Nicolas Milon, Mari D. Heghinian et al. 59 citations

Noribogaine is the long-lived human metabolite of the anti-addictive substance ibogaine. Noribogaine efficaciously reaches the brain with concentrations up to 20 μM after acute therapeutic dose of 40 mg/kg ibogaine in animals. Noribogaine displays atypical opioid-like components in vivo, anti-addictive effects and potent modulatory properties of the tolerance to opiates for which the mode of...

Noribogaine is a Mixed Agonist/Antagonist Opioid Ligand with Profound Functional Selectivity

The FASEB Journal April 1, 2015 Émeline L. Maillet, Nicolas Milon, James A. Fishback et al. 1 citation

Noribogaine is the primary metabolite of the anti‐addictive substance ibogaine, which modulates opiate analgesic activity and the components of drug addiction in animal models at brain concentrations of 0.5‐15 µM. In this study, molecular activities of noribogaine at mu (OPRM) and kappa (OPRK) opioid receptors were characterized. Noribogaine was a moderately potent antagonist of the OPRM...

Characterization of Noribogaine at nAChRs and Effect on Nicotine Self‐Administration in Rats

The FASEB Journal April 1, 2015 Émeline L. Maillet, Qing Chang, Nicolas Milon et al.

Noribogaine, a polypharmacological drug with activities at opioid receptors, ionotropic nicotinic receptors, and serotonin reuptake transporters, is being investigated for treatment of substance abuse‐related disorders. In this study, noribogaine molecular activity at neuronal nicotinic acetylcholine receptors (nAChRs) was characterized. Noribogaine inhibited α3β4, α7 nAChRs, and endogenously...