Jan Kehler

2 papers in the library · 3 citations · publishing 2016-2025

Papers

Are the LSD-analogs lisuride and ergotamine examples of non-hallucinogenic serotonin 5-HT2A receptor agonists?

Journal of psychopharmacology (Oxford, England) May 5, 2025 Jan Kehler, Morten Skøtt Thomsen Lindskov 3 citations

A review of the literature on 5-HT2A receptor agonists, including psychedelics like LSD and the supposedly non-hallucinogenic compounds lisuride and ergotamine, finds no evidence that lisuride or ergotamine are non-hallucinogenic at relevant brain concentrations. This challenges the assumption that altered states of consciousness are not a prerequisite for therapeutic effects. The authors caution against relying solely on animal data when developing non-hallucinogenic 5-HT2A receptor agonists and emphasize the need for rigorous human studies to confirm target engagement before claiming a compound is non-hallucinogenic.

DOI: 10.1177/02698811251330741 Full text LSD Serotonin Lisuride Psychedelics hallucinogens +6

5-HT2A/5-HT2C Receptor Pharmacology and Intrinsic Clearance of N-Benzylphenethylamines Modified at the Primary Site of Metabolism.

ACS Chemical Neuroscience November 16, 2016 Sebastian Leth-Petersen, Ida N Petersen, Anders A. Jensen et al.

The toxic hallucinogen 25B-NBOMe is rapidly broken down by human liver enzymes and has low oral bioavailability. New chemical variants were synthesized by modifying the part of the molecule where metabolism normally occurs. While some analogues resisted breakdown longer and still strongly activated 5-HT2 receptors, all had an intrinsic clearance above 1.3 L/kg/h, indicating they would still be extensively metabolized on first pass through the liver.

DOI: 10.1021/acschemneuro.6b00265 Full text 5-ht2a receptor agonists Phenethylamines Hallucinogens Microsomal stability