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Home/Research/Mescaline/Medicinal Chemistry & Drug Development

Mescaline for Medicinal Chemistry & Drug Development

9 papers and 0 clinical trials exploring mescaline as a treatment for medicinal chemistry & drug development.

CompoundPhenethylamine

Mescaline

A naturally occurring phenethylamine psychedelic found in certain cacti, investigated for its role in religious practice and psychiatric research.

Full Mescaline 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

9 papers
Paywallindividual

Pharmacokinetics, Pharmacodynamics, and Urinary Recovery of Oral Mescaline Hydrochloride in Healthy Participants

This pharmacokinetic-pharmacodynamic analysis (n=46) of two Phase I trials of oral mescaline (100-800 mg) showed dose-proportional exposure with peak concentrations at 2 hours, a half-life of 3.5 hours, onset of effects around 1 hour post-dose, maximum effect intensity and duration ranging from 13% and 2.8 hours (100 mg) to 89% and 15 hours (800 mg), with 53% urinary excretion unchanged and 31% as the main metabolite, indicating at least 53% oral bioavailability.

Published
July 14, 2025
Journal
Clinical Pharmacokinetics
Authors
Mueller, L., Klaiber, A., Ley, L., Becker, A. M., Thomann, J., Luethi, D., Schmid, Y., Liechti, M. E.
Open Accessindividual

Acute dose-dependent effects of mescaline in a double-blind placebo-controlled study in healthy subjects

In a randomized double‑blind placebo‑controlled crossover study in 16 healthy volunteers, oral mescaline (100–800 mg) produced dose‑dependent subjective and autonomic effects with dose‑proportional pharmacokinetics (Tmax ≈2 h, t1/2 ≈3.5 h) and increasing duration (6.4–14 h), with reduced tolerability and frequent nausea/emesis at 800 mg. Co‑administration of the 5‑HT2A antagonist ketanserin markedly attenuated and shortened the effects of 800 mg mescaline, indicating that its acute effects are primarily mediated by 5‑HT2A receptors.

Published
September 30, 2024
Journal
Translational Psychiatry
Authors
Klaiber, A., Schmid, Y., Becker, A. M., Straumann, I., Erne, L., Jelusic, A., Thomann, J., Luethi, D., Liechti, M. E.
Open Accessmeta

Drug-drug interactions involving classic psychedelics: A systematic review

This systematic review of 52 human studies summarises drug–drug interactions between classic psychedelics (LSD, psilocybin, mescaline, DMT, 5‑MeO‑DMT) and various psychotropic and recreational drugs, finding heterogeneous outcomes — attenuated, potentiated or unchanged effects — with few serious adverse events reported beyond isolated case reports. The paper provides a comprehensive synthesis of clinical evidence and discusses potential molecular mechanisms underlying these interactions.

Published
November 20, 2023
Journal
Journal of Psychopharmacology
Authors
Halman, A., Kong, G., Sarris, J., Perkins, D.
Open Accessindividual

Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines

This study characterises the receptor profiles of 4-alkoxy-3,5-dimethoxy phenethylamines (scalines) and their amphetamine analogues (3C-scalines), finding they interact primarily with 5-HT2A and 5-HT2C receptors with weak-to-moderate affinity but up to 63‑fold and 34‑fold higher binding than mescaline. Extension or fluorination of the 4‑alkoxy substituent increased 5‑HT2A/2C affinity and 5‑HT2A activation potency, while non-serotonergic monoamine targets showed little potency.

Published
February 9, 2022
Journal
Frontiers in Pharmacology
Authors
Kolaczynska, K. E., Luethi, D., Trachsel, D., Hoener, M. C., Liechti, M. E.
Open Accessindividual

Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

This study reveals structurally how psychedelics, including LSD, psilocin, mescaline, and various N-BOH analogs, mediate their therapeutic and hallucinogenic effects by binding to and activating their molecular target, the serotonin (5-HT) 2A receptor coupled with G-protein Gaq.

Published
September 1, 2020
Journal
Cell
Authors
Kim, K., Che, T., Panova, O., Shoichet, B. K., Skiniotis, G., Roth, B. L., Diberto, J. F., Lyu, J., Krumm, B. E., Wacker, D., Robertson, M. J., Seven, A. B., Nichols, D. E.
Paywallindividual

Correlation between the potency of hallucinogens in the mouse head-twitch response assay and their behavioral and subjective effects in other species

This mouse study investigates the correlation between the hallucinogens potency in the mouse head-twitch response (HTR) paradigm and their reported potencies in other species such as rats and humans. It used dose-response studies with psychedelics in mice and found a very strong correlation (r=0.95) with earlier human data (n=36).

Published
May 1, 2020
Journal
Neuropharmacology
Authors
Halberstadt, A. L., Chatha, M., Klein, A. K., Wallach, J., Brandt, S. D.

Clinical Trials

0 trials

No clinical trials have been tagged with both Mescaline and Medicinal Chemistry & Drug Development yet.

Trials are continuously being added as new studies are registered.

Explore further

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