Synthesis and In Vitro Profiling of Psilocin Derivatives : Improved Stability and Synthetic Properties
(2025) In Journal of Medicinal Chemistry 68(7). p.7153-7165- 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,... (More)
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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- author
- Eklund, Julia ; Bremberg, Ulf ; Larsson, Jessica ; Torkelsson, Edvard ; Wennerberg, Johan LU ; Zandelin, Symantha and Odell, Luke R.
- organization
- publishing date
- 2025-04
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Journal of Medicinal Chemistry
- volume
- 68
- issue
- 7
- pages
- 13 pages
- publisher
- The American Chemical Society (ACS)
- external identifiers
-
- pmid:40108981
- scopus:105000222846
- ISSN
- 0022-2623
- DOI
- 10.1021/acs.jmedchem.4c02612
- language
- English
- LU publication?
- yes
- id
- eda553f0-a4f1-4857-a99f-201ae6b5f2cd
- date added to LUP
- 2026-01-12 13:05:19
- date last changed
- 2026-01-13 03:00:18
@article{eda553f0-a4f1-4857-a99f-201ae6b5f2cd,
abstract = {{<p>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.</p>}},
author = {{Eklund, Julia and Bremberg, Ulf and Larsson, Jessica and Torkelsson, Edvard and Wennerberg, Johan and Zandelin, Symantha and Odell, Luke R.}},
issn = {{0022-2623}},
language = {{eng}},
number = {{7}},
pages = {{7153--7165}},
publisher = {{The American Chemical Society (ACS)}},
series = {{Journal of Medicinal Chemistry}},
title = {{Synthesis and In Vitro Profiling of Psilocin Derivatives : Improved Stability and Synthetic Properties}},
url = {{http://dx.doi.org/10.1021/acs.jmedchem.4c02612}},
doi = {{10.1021/acs.jmedchem.4c02612}},
volume = {{68}},
year = {{2025}},
}