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Home/Research/Psilocybin/Medicinal Chemistry & Drug Development

Psilocybin for Medicinal Chemistry & Drug Development

34 papers and 3 clinical trials exploring psilocybin as a treatment for medicinal chemistry & drug development.

CompoundClassic Psychedelic

Psilocybin

Psilocybin is a naturally occurring tryptamine psychedelic that acts as a prodrug to psilocin, a potent 5-HT2A receptor agonist. It is the furthest advanced psychedelic in clinical development, with two positive Phase III trials in treatment-resistant depression and expanding regulated access in Australia, Germany, and US states.

Full Psilocybin profile
IndicationOver 300 million people worldwide experience depression, with many also suffering from related anxiety disorders.

Medicinal Chemistry & Drug Development

Medicinal chemistry plays a crucial role in the development of novel psychedelic compounds, focusing on their molecular structures and interactions. Researchers utilise innovative methods to enhance safety and efficacy in psychedelic substances.

Full Medicinal Chemistry & Drug Development profile

Academic Research

34 papers
Open Accessindividual

Serotonergic Polypharmacology of 2-Halogenated Tryptamines

This mouse study found that 2-halogenated tryptamine derivatives of DMT and psilocybin had reduced activity at receptors linked to psychedelic effects and heart-related risks, while keeping strong activity at 5-HT6 receptors. In mice, 2-Br-psilacetin did not trigger the usual head-twitch response and showed some improvements in stress-related behaviour and cued learning.

Published
April 21, 2026
Journal
Biorxiv
Authors
Yacoub, J., Bray, E., Bayyat, J., Glatfelter, G. C., Leake, A., Buitrago, E. M., Maitland, A. D., Partilla, J., Cavalco, N. G., Schalk, S. S., Lammers, J. C., Baumann, M. H., McCorvy, J., Leahy, J. W., Gulick, D., Witowski, C. G., von Salm, J. L.
Open Accessindividual

A novel psychedelic 5-HT2A receptor agonist GM-2505: The pharmacokinetic, safety, and pharmacodynamic profile from a randomized trial healthy volunteer

In a randomized, placebo‑controlled ascending‑dose study in 48 healthy volunteers, single IV doses of GM‑2505 up to 20 mg were well tolerated and showed dose‑proportional pharmacokinetics (t1/2 40–50 min) with dose‑dependent neuroendocrine, neurophysiological and subjective psychedelic effects, including decreased theta/alpha and increased gamma EEG power. The duration of cardiovascular and subjective effects was intermediate between psilocybin and DMT, indicating a practical 10–15 mg IV dose range for supervised clinical use.

Published
October 16, 2025
Journal
Journal of Psychopharmacology
Authors
Marek, G. J., Makai-Bölöni, S., Umbricht, D., Christian, E. P., Winters, J., Dvorak, D., Raines, S., Hughes, Z. A., Austin, E. W., Klein, A. K., Leong, W., Krol, F. J., Van Der Graaf, A. J., Juachon, M. J., Otto, M. E., Borghans, L. G. J. M., Jacobs, G., Kruegel, A. C., Sporn, J.
Paywallindividual

Zalsupindole is a Nondissociative, Nonhallucinogenic Neuroplastogen with Therapeutic Effects Comparable to Ketamine and Psychedelics

This rat study found that zalsupindole (third-generation psychedelic) produced robust effects on structural and functional neuroplasticity in the prefrontal cortex as well as sustained antidepressant-like responses comparable to or greater than those of ketamine, psilocybin, and DMT, despite lacking any of the acute cellular and behavioural characteristics of hallucinogenic or dissociative compounds.

Published
October 13, 2025
Journal
ACS Chemical Neuroscience
Authors
Agrawal, R., Gillie, D., Mungenast, A., Chytil, M., Engel, S., Wu, M. C., Rasmussen, K., Salinas, E., Olson, D. E.
Open Accessindividual

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Subcutaneous RE104: A Double-Blind, Randomized, Single Ascending Dose Placebo-Controlled Study

This double-blind, randomised, placebo-controlled Phase I study (n=48) evaluates the safety, pharmacokinetics, and psychoactive effects of RE104 (psilocybin analog; Luvesilocin; a prodrug of 4-OH-DiPT) in healthy adults with prior psychedelic experience. RE104 was well tolerated up to 40 mg with no serious adverse events, and plasma levels of its active form correlated with subjective drug effect and mystical experience scores. The compound produced psilocybin-like effects with a shorter duration (3-4 hours), supporting further therapeutic investigation.

Published
July 21, 2025
Journal
Journal of Clinical Psychopharmacology
Authors
Ludbrook, G., Bryson, N., Taylor, B., Hocevar-Trnka, J., Johnson, M. W., Hirman, J., Morrish, G., Alexander, R., Pollack, M.
Open Accessindividual

Assessing the Potential Cardiovascular Risk of Microdosing the Psychedelic LSD in Mice

Chronic administration of sub‑hallucinogenic (microdose) LSD in mice produced no ventricular thickening or other ECG-detected cardiotoxic changes, whereas serotonin (positive control) caused significant ventricular thickening. In vitro assays showed similar 5‑HT2B affinity across mouse and human receptors and that low‑dose LSD yields only transient 5‑HT2B activation compared with the cardiotoxin d‑fenfluramine, together providing no evidence of cardiovascular risk from prolonged low‑dose LSD in this mouse model.

Published
April 14, 2025
Journal
ACS Pharmacology and Translational Science
Authors
Effinger, D. P., Schalk, S. S., King, J. L., Wallingford, J. R., O'connell, C. K., Calderon, J. R., Kopecky, B. J., Mccorvy, J. D., Thompson, S. M.
Open Accessindividual

Acute Effects and Pharmacokinetics of LSD after Paroxetine or Placebo Pre-Administration in a Randomized, Double-Blind, Cross-Over Phase I Trial

In a randomized, double‑blind, cross‑over trial in 23 healthy volunteers, daily paroxetine (a CYP2D6 inhibitor) did not change LSD's pleasant subjective effects but significantly reduced adverse effects (bad drug effect, anxiety, nausea) and increased LSD Cmax and AUC by ~1.4–1.5-fold. The findings indicate CYP2D6 contributes to LSD metabolism and suggest co‑administration with SSRIs that inhibit CYP2D6 is well tolerated and likely does not require LSD dose adjustment, although recommendations for SSRIs that do not inhibit CYP2D6 remain uncertain.

Published
February 28, 2025
Journal
Clinical Pharmacology and Therapeutics
Authors
Becker, A. M., Humbert-Droz, M., Mueller, L., Jelusic, A., Tolev, A., Straumann, I., Avedisian, I., Erne, L., Thomann, J., Luethi, D., Grünblatt, E., Meyer zu Schwabedissen, H. E., Liechti, M. E.

Clinical Trials

3 trials
CompletedPhase I

A Study Assessing Brain Activity, Safety, Tolerability, and Pharmacokinetics Following Multiple Doses of MLS101 (Psilocybin) in Healthy Volunteers

This Phase I randomised, single-blind trial (n=20) will study the effects of multiple low doses of psilocybin (MLS101) on brain activity, safety, tolerability, and pharmacokinetics in healthy adult volunteers.

Started
July 1, 2025
Type
interventional
Blinding
single
Randomized
Yes
Registry ID
NCT07050368
CompletedPhase I

A study in healthy male volunteers to investigate how the test medicine COMP360 [14C]-psilocybin is taken up, broken down and removed from the body

This Phase I, open-label trial (n=6) investigates how psilocybin (COMP360; 10mg) is absorbed, distributed, metabolised, and excreted in healthy male volunteers aged 30-55.

Started
July 18, 2024
Type
interventional
Blinding
none
Randomized
No
Registry ID
ISRCTN37167117
CompletedPhase I

A phase I, open-label, randomised-sequence, two-way crossover study to assess the relative oral bioavailability of 25 mg and 5 mg strength capsules of COMP360 in healthy volunteers

Phase I open-label randomised two-way crossover PK study in healthy volunteers (n=14) comparing 25 mg COMP360 as a single 25 mg capsule versus five 5 mg capsules in the fed state.

Started
October 24, 2022
Type
interventional
Blinding
none
Randomized
Yes
Registry ID
ISRCTN16636661

Explore further

Search all Psilocybin papers Search all Medicinal Chemistry & Drug Development trials Full Psilocybin profile Full Medicinal Chemistry & Drug Development profile