Frontiers in pharmacology
January 1, 2019
Soledad Marton, Bruno González, Sebastián Rodríguez-bottero et al.
71 citations
A single injection of ibogaine in rats increased the expression of neurotrophic factors in brain regions containing dopamine neurons, with effects depending on dose and brain area. At 24 hours, the higher dose (40 mg/kg) selectively raised GDNF in the ventral tegmental area and substantia nigra, while both doses boosted BDNF transcripts in the nucleus accumbens, substantia nigra, and prefrontal cortex. NGF mRNA increased across all regions after the higher dose. Protein levels showed GDNF rise only in the ventral tegmental area at the higher dose, and proBDNF increased in the nucleus accumbens for both doses. These changes may help explain ibogaine's reported ability to reduce drug-seeking behavior.
Frontiers in pharmacology
January 1, 2018
Joaquín González, José P Prieto, Paola Rodríguez et al.
31 citations
Ibogaine, a psychedelic alkaloid with anti-addictive properties, acutely increases wakefulness and suppresses REM sleep in rats. In a study with polysomnographic recordings over six hours, rats given ibogaine (20 or 40 mg/kg) spent more time awake and less time in slow wave sleep and REM sleep compared to controls. REM sleep latency increased with the higher dose. The wake-promoting and slow wave sleep effects occurred in the first two hours, while REM suppression lasted throughout the recording. Lower doses increased locomotion; higher doses caused tremor and flat body posture. Head shake response, linked to 5HT2A receptor activation, was unchanged. The findings suggest ibogaine produces a waking state with prolonged REM suppression and a dose-dependent motor profile.
ACS Omega
April 1, 2022
Luisina Castelli Rodríguez, Andrés Mariño López, Guillermo Moyna et al.
28 citations
Ayahuasca, a psychedelic beverage from the Amazon, is made by boiling Banisteriopsis caapi vine with DMT-containing plants. Using NMR and LC-MS/MS, this study analyzed both soluble and insoluble components of ayahuasca samples. For the first time, fructose was detected as a major component, and the alkaloid harmine was found in suspended solids. The major alkaloids identified were DMT, harmine, tetrahydroharmine, harmaline, and harmol. A new quantitative NMR method was developed and validated to simultaneously quantify these alkaloids.
Journal of natural products
June 23, 2023
Bruno González, Nicolás Veiga, Gonzalo Hernández et al.
7 citations
The iboga alkaloids, such as ibogaine and voacangine, are promising scaffolds for developing drugs to treat neuropsychiatric disorders. This work examines how these molecules react under oxidation with dioxygen, peroxo compounds, and iodine. The C16-carboxymethyl ester group in voacangine makes the molecule more stable toward oxidation than ibogaine, particularly in the indole ring, where 7-hydroxy- or 7-peroxy-indolenines form. However, the ester increases reactivity at the isoquinuclidinic nitrogen, leading to C3-oxidized products via regioselective iminium formation. Density functional theory calculations explain this differential reactivity. Additionally, NMR experiments and theoretical calculations revise the absolute stereochemistry at C7 in voacangine's 7-hydroxyindolenine to S, correcting earlier reports of R configuration.
ChemRxiv
October 29, 2018
Soledad Marton, Bruno González, Sebastián Rodríguez et al.
Ibogaine, a psychedelic alkaloid, alters the expression of three neurotrophic factors—GDNF, BDNF, and NGF—in rat brain regions containing dopamine neurons. A single injection of 20 or 40 mg/kg ibogaine increased expression of these factors after 24 hours in a dose- and region-specific manner. The higher dose selectively raised GDNF in the ventral tegmental area and substantia nigra. Both doses increased BDNF in the nucleus accumbens, substantia nigra, and prefrontal cortex, while the higher dose also raised BDNF in the ventral tegmental area. NGF increased in all regions after the higher dose. Mature GDNF protein rose in the ventral tegmental area, and proBDNF increased in the nucleus accumbens. These changes may contribute to ibogaine's anti-addictive properties.