Tabernanthalog Explained

Tabernanthalog (TBG, DLX-007)[1] is a novel water-soluble, non-toxic azepinoindole[2] analog of the psychoactive drug Tabernanthine first synthesized by Professor David E. Olson at UC Davis.

Tabernanthalog is a non-hallucinogenic serotonin 5-HT2A receptor agonist.[3] It is also a serotonin 5-HT2B receptor antagonist. The drug is described as having high selectivity for the serotonin 5-HT2 receptors. Other targets of the drug include monoamine oxidase A (MAO-A), the α2A-adrenergic receptor, the serotonin 5-HT1B and 5-HT2C receptors, and the serotonin transporter (SERT).

In rodents, it was found to promote structural neural plasticity, reduce drug seeking behavior, and produce antidepressant like effects.[4] [5] It has also been shown that it effectively reduces motivation for heroin and alcohol in rats. This indicates its efficacy in animals with a history of heroin and alcohol polydrug use.[6]

Due to the rapidly-induced and enduring neuroplasticity, tabernanthalog is a member of the class of compounds known as non-hallucinogenic psychoplastogens. This compound, as well as related compounds, are licensed by Delix Therapeutics and are being developed as potential medicines for neuropsychiatric disorders.[7]

See also

Notes and References

  1. Cameron LP, Tombari RJ, Lu J, Pell AJ, Hurley ZQ, Ehinger Y, Vargas MV, McCarroll MN, Taylor JC, Myers-Turnbull D, Liu T, Yaghoobi B, Laskowski LJ, Anderson EI, Zhang G, Viswanathan J, Brown BM, Tjia M, Dunlap LE, Rabow ZT, Fiehn O, Wulff H, McCorvy JD, Lein PJ, Kokel D, Ron D, Peters J, Zuo Y, Olson DE . 6 . A non-hallucinogenic psychedelic analogue with therapeutic potential . Nature . 589 . 7842 . 474–479 . January 2021 . 33299186 . 7874389 . 10.1038/s41586-020-3008-z . 2021Natur.589..474C .
  2. Hester JB, Tang AH, Keasling HH, Veldkamp W . Azepinoindoles. I. Hexahydroazepino[4,5-b]indoles . Journal of Medicinal Chemistry . 11 . 1 . 101–106 . January 1968 . 5637151 . 10.1021/jm00307a023 .
  3. Cameron LP, Tombari RJ, Lu J, Pell AJ, Hurley ZQ, Ehinger Y, Vargas MV, McCarroll MN, Taylor JC, Myers-Turnbull D, Liu T, Yaghoobi B, Laskowski LJ, Anderson EI, Zhang G, Viswanathan J, Brown BM, Tjia M, Dunlap LE, Rabow ZT, Fiehn O, Wulff H, McCorvy JD, Lein PJ, Kokel D, Ron D, Peters J, Zuo Y, Olson DE . A non-hallucinogenic psychedelic analogue with therapeutic potential . Nature . 589 . 7842 . 474–479 . January 2021 . 33299186 . 7874389 . 10.1038/s41586-020-3008-z .
  4. Lu J, Tjia M, Mullen B, Cao B, Lukasiewicz K, Shah-Morales S, Weiser S, Cameron LP, Olson DE, Chen L, Zuo Y . 6 . An analog of psychedelics restores functional neural circuits disrupted by unpredictable stress . Molecular Psychiatry . 26 . 11 . 6237–6252 . November 2021 . 34035476 . 8613316 . 10.1038/s41380-021-01159-1 .
  5. Peters J, Olson DE . Engineering Safer Psychedelics for Treating Addiction . Neuroscience Insights . 16 . 26331055211033847 . 2021-07-20 . 34350400 . 8295933 . 10.1177/26331055211033847 .
  6. Heinsbroek JA, Giannotti G, Bonilla J, Olson DE, Peters J . Tabernanthalog Reduces Motivation for Heroin and Alcohol in a Polydrug Use Model . Psychedelic Medicine . 1 . 2 . 111–119 . June 2023 . 37360328 . 10.1089/psymed.2023.0009 . 10286262 .
  7. Grace B . 6 March 2021 . Can we take the high out of psychedelics? . Wired . 12 July 2022.

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