Synthesis and In Vitro Profiling of Psilocin Derivatives: Improved Stability and Synthetic Properties

As interest in using psilocybin therapy for treating mental health disorders intensifies, the need for efficient production methods becomes increasingly important. Current medical-grade psilocybin production is inefficient and relies on a complicated multistep synthesis. This study has explored and evaluated psilocin ester prodrugs and psilocin salts as potential alternatives to psilocybin, focusing on their ease of synthesis, chemical stability, and metabolic profiles. A diverse library of 15 psilocin ester prodrugs and six psilocin salts was synthesized and evaluated. The study successfully identified several psilocin ester prodrugs and psilocin salts that exhibited desirable characteristics, including storage and handling stability, rapid metabolic conversion to psilocin, and easy synthesis, with potential advantages over psilocybin. This research introduces viable options through psilocin ester compounds and psilocin salts, offering promising avenues for future development.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2025-03-20
DOI
https://doi.org/10.1021/acs.jmedchem.4c02612
Citations
2
Primary Topic
Psychedelics and Drug Studies
Type
article
Field-Weighted Citation Impact
4.61

Funders

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article

Synthesis and In Vitro Profiling of Psilocin Derivatives: Improved Stability and Synthetic Properties

Edvard Torkelsson, Jessica Larsson, Ulf Bremberg, Luke R. Odell et al.
2 citations
Journal of Medicinal Chemistry
Psychedelics and Drug Studies
4.61
article

Synthesis and In Vitro Profiling of Psilocin Derivatives: Improved Stability and Synthetic Properties

Edvard Torkelsson, Jessica Larsson, Ulf Bremberg, Luke R. Odell, Johan Wennerberg, Jesper Eklund, Symantha Zandelin
article en
2 citations

Abstract

As interest in using psilocybin therapy for treating mental health disorders intensifies, the need for efficient production methods becomes increasingly important. Current medical-grade psilocybin production is inefficient and relies on a complicated multistep synthesis. This study has explored and evaluated psilocin ester prodrugs and psilocin salts as potential alternatives to psilocybin, focusing on their ease of synthesis, chemical stability, and metabolic profiles. A diverse library of 15 psilocin ester prodrugs and six psilocin salts was synthesized and evaluated. The study successfully identified several psilocin ester prodrugs and psilocin salts that exhibited desirable characteristics, including storage and handling stability, rapid metabolic conversion to psilocin, and easy synthesis, with potential advantages over psilocybin. This research introduces viable options through psilocin ester compounds and psilocin salts, offering promising avenues for future development.

Journal of Medicinal ChemistryVol. 68(7)
Uppsala University (SE), Lund University (SE), Medicon Village (SE), Red Glead Discovery (Sweden) (SE)
Hjärnfonden, Vetenskapsrådet, Uppsala Universitet
Openalex Percentile: Top 7%
Psychedelics and Drug Studies
4.61
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Synthesis and In Vitro Profiling of Psilocin Derivatives: Improved Stability and Synthetic Properties — Edvard Torkelsson, Jessica Larsson, et al. · Journal of Medicinal Chemistry (2025) | TGRS Research Map | TGRS