ArticleJournal of medicinal chemistry2024
Novel Psilocin Prodrugs with Altered Pharmacological Properties as Candidate Therapies for Treatment-Resistant Anxiety Disorders.
Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 17 citations in OpenAlex.
- Psilocybin, From Ancestral Use to Therapeutic Potential: A Multidimensional Review of Its Pharmacological Basis and Current Perspectives.Human psychopharmacology · 2026Review
- Synthesis and Biological Evaluation of 4‑Bromo-ACS omega · 2026Article
- Psilocybin improves novel object recognition in a rat model of Fragile X Syndrome through the modulation of the BDNF/TrkB signaling pathway.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- RGReco: a unified framework for automated R-group recognition in chemical publications.Journal of cheminformatics · 2026Article
- Design, Synthesis, and Pharmacokinetic Profiling of Fluorinated ReversibleJournal of medicinal chemistry · 2026Article
- Difficult-to-Treat Anxiety: A Neurocomputational Framework.Biological psychiatry. Cognitive neuroscience and neuroimaging · 2025Review
- Efficient Acyloxymethylation of Psilocin and Other Tryptamines Yielding ACOM Prodrugs for Psychedelic-Assisted Therapy.Archiv der Pharmazie · 2025Article
- Synthesis and In Vitro Profiling of Psilocin Derivatives: Improved Stability and Synthetic Properties.Journal of medicinal chemistry · 2025Article
- Pharmacokinetics of Psilocybin: A Systematic Review.Pharmaceutics · 2025Review
- Extraction Yields of Psilocybin and Psilocin: A Short Review of Current Methods and Their Implications.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Psilocybin for the treatment of Alzheimer's disease.Frontiers in neuroscience · 2024Review
Corrections and comments
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Authors and funding
15 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The psychedelic prodrug psilocybin has shown therapeutic benefits for the treatment of numerous psychiatric conditions. Despite positive clinical end points targeting depression and anxiety, concerns regarding the duration of the psychedelic experience produced by psilocybin, associated with enduring systemic exposure to the active metabolite psilocin, pose a barrier to its therapeutic application. Our objective was to create a novel prodrug of psilocin with similar therapeutic benefits but a reduced duration of psychedelic effects compared with psilocybin. Here, we report the synthesis and functional screening of 28 new chemical entities. Our strategy was to introduce a diversity of cleavable groups at the 4-hydroxy position of the core indole moiety to modulate metabolic processing. We identified several novel prodrugs of psilocin with altered pharmacokinetic profiles and reduced pharmacological exposure compared with psilocybin. These candidate prodrugs have the potential to maintain the long-term benefits of psilocybin therapy while attenuating the duration of psychedelic effects.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.